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دانلود کتاب ENCYCLOPEDIA OF MOLECULAR PHARMACOLOGY
دانلود کتاب دایره المعارف فارماکولوژی مولکولی
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ENCYCLOPEDIA OF MOLECULAR PHARMACOLOGY
ویرایش: [3 ed.] سری: ISBN (شابک) : 9783030574017, 3030574016 ناشر: SPRINGER سال نشر: 2021 تعداد صفحات: [1625] زبان: English فرمت فایل : PDF (درصورت درخواست کاربر به PDF، EPUB یا AZW3 تبدیل می شود) حجم فایل: 52 Mb
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Preface to the Third Edition Preface to the Second Edition Preface to the First Edition List of Topics About the Editors Contributors A A Receptors AADs, Antiarrhythmic Agents ABC Proteins ABC Transporters Synonyms Definition Basic Characteristics Topology and Structure Tissue Distribution and Localization Physiological and Pathophysiological Aspects Drugs Drug Transport References 7-ACA Derivatives ACE Inhibitors Synonyms Angiotensin-1 Converting Enzyme (ACE) Mechanism of Action of ACE Inhibitors Molecular Properties of ACE Design of First-Generation ACE Inhibitors Adverse Effects of Present ACE Inhibitors ACE Inhibitors: Clinical Implications Essential Hypertension Congestive Heart Failure and Myocardial Infarction Diabetic Nephropathy ACE Inhibitors and Cancer ACE Inhibitors as Modulators of Atherosclerosis New Generation of Domain-Specific ACE Inhibitors Dual ACE/NEP or Vasopeptidase Inhibitors Acknowledgments References Acetylcholine Acetylhydrolase Acetylcholine Hydrolase Acetylcholinesterase (EC 3.1.1.7) (AChE) Acetylthiocholinesterase Acetyl-β-Methylcholinesterase Acid-Sensing Ion Channels Definition Basic Characteristics Channel Family Structural Organization Basic Functional Properties Physiological Roles ASIC Regulators Ions and Polyamines Neuropeptides Proteases Protein Kinases Amphiphilic Substances Lipids GMQ and Related Compounds Drugs Toxins Small Molecule Inhibitors References Acylcholine Acylhydrolase Adaptor Proteins Synonyms Definition Basic Mechanisms Adaptor Protein Function Assembly of Signaling Complexes Spatial Regulation Temporal Regulation Activation of Signaling Components Inactivation of Kinases Sequestering Signaling Components Domains Src Homology 2 (SH2) and Src Homology 3 (SH3) Postsynaptic Density Protein/Drosophila Disk Large Tumor Suppressor/Zonula Occludens-1 Protein (PDZ) Phosphotyrosine Binding (PTB) WW Pleckstrin Homology (PH) Regulation of Adaptor Proteins Phosphorylation Chemical Regulation Intramolecular Interactions Conformational Changes Pharmacological Intervention References ADC ADCs Adenosine Receptors Synonyms Definition Basic Characteristics Sources of Adenosine, Its Transport Mechanisms, and Metabolism Signaling Pathways Coupled to ARs and AR Regulation Selective Ligands and Indirect Modulators of Adenosine Signaling Agonists Antagonists Radioligands Receptor Structures Drugs References Adenyl Cyclase (Original) Adenyl Cyclase (Preferred) Adenylate Cyclase (Not Chemically Correct) Adenylyl Cyclases Synonyms Definition Basic Characteristics and Mechanisms Classes of Adenylyl Cyclases Mammalian Adenylyl Cyclases Catalytic Mechanism Miscellaneous Observations Bacterial and Other Adenylyl Cyclases Drugs Cellular Inhibition of AC References Adipocyte-Derived Factors Adipocytokines Adipokines Synonyms Definition Basic Characteristics Adipose Tissue as an Endocrine Organ Leptin: An Adipokine Dysregulated in Obesity Which Influences Appetite, Body Weight, and Vascular Function Adiponectin: Insulin Sensitizer and Potential Endothelial Protector FABP4: Lipid Transport Protein Implicated in Several Aspects of the Metabolic Syndrome FGF21: Beneficial Effects on Glucose and Lipid Metabolism in Multiple Target Organs BMP7: An Adipokine that Induces Brown Adipogenesis and Reduces Food Intake and Weight Gain Chemerin: Multifaceted Adipokine Displays Various Roles in the Pathogenesis of Inflammation and Metabolic Disease Fetuin-A: Circulating Protein Linked to Insulin Resistance and Obesity GDF15: Stress Response Cytokine with Impact on Energy Homeostasis IL-1β: Inflammatory Marker of Obesity TNF-α: Inflammatory Marker of Obesity Omentin: A Biomarker of Metabolic Disorders Drugs References Ado Receptors α-Adrenergic Receptors α-Adrenergic System Synonyms Definition Basic Characteristics Drugs References α-Adrenoceptors Adrenomedullin Receptor Adrenomedullin/Intermedin Synonyms/Abbreviations Definition Basic Characteristics Pharmacology Physiology, Pathophysiology, and Therapeutic Potential References Advanced Glycation End-Proteins Definition Basic Mechanisms General AGEs and Diseases Diagnostic Opportunities Pharmacological Intervention References AGTRL1 Ligand A-Kinase Anchoring Proteins (AKAPs) Synonyms Definition Basic Mechanisms AKAP-Dependent Control of cAMP/PKA Signaling AKAP-PKA Binding AKAP-Dependent Integration of Cellular Signaling AKAPs Optimize the Limited Repertoire of Cellular Signaling Proteins Pharmacological Intervention References Alcohol Dependence Alkali Cation/Proton Antiporter Alkali Cation/Proton Exchanger Allergy Alzheimer´s Dementia Alzheimer´s Disease Synonyms Definition Basic Mechanisms General Sporadic Alzheimer´s Disease Familial Alzheimer´s Disease Aβ Production, Clearance, and Aggregation Amyloid Hypothesis Pharmacological Intervention General Symptomatic Treatment Approaches Toward Disease-Modifying Treatment Cross-References References AMP-Activated Protein Kinase Synonyms Definition Basic Characteristics Structure Regulation Canonical Regulation by Adenine Nucleotides Noncanonical Regulation by Hormones Involved in Regulation of Whole-Body Energy Balance Noncanonical Activation by Glucose Starvation Downstream Targets of AMPK Drugs Agents That Act Indirectly by Inhibiting Mitochondrial Function Prodrugs That Are Converted by Cellular Metabolism into AMP Analogs Agents That Activate AMPK by Binding the Allosteric Drug and Metabolite (ADaM) Site References AMPK Amylin Synonyms Definition Basic Characteristics Physiological Role Glucose Regulation Satiety Adiposity Signal Energy Expenditure Pathological Roles Islet Amyloid and T2D Progression Human Amylin and Alzheimer´s Disease Amylin Receptors Drugs Amylin Receptor Agonist-Based Drugs Approved Drugs Exploratory Drugs Amylin Aggregation Inhibitor-Based Drug Cross-References References Amylin Receptor Anakinra Analgesics Synonyms Definition Mechanisms of Action Opioids Nonsteroidal Anti-inflammatory Drugs (NSAIDs) Antiepileptics Antidepressants/Serotoninergic Drugs Clinical Use and Side Effects Opioids NSAIDs Antiepileptics Antidepressants/Serotoninergic Drugs Other Drugs References Anchoring Protein Angiotensin-1 Converting Enzyme Inhibitors Anion Channels Anomalous Rectifiers Anterograde Amnesia Antiarrhythmic Drugs Synonyms Definition Basic Characteristics Clinical Use Mechanisms of Action Antiarrhythmic Mechanisms (Proarrhythmic) Side Effects Molecular Targets Drugs Class 0: Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channel Blockers Class I: Na+ Channel Blockers Class II: Autonomic Inhibitors Class III: K+ Channel Blockers Class IV: Ca2+ Channel Blockers and Ca2+-Handling Modulators Classes V-VII Conclusion References Antibody Drug Conjugates Synonyms Definition Mechanism of Action Clinical Use References Anticoagulants Synonyms Definition Mechanism of Action Indirect Thrombin Inhibitors Direct Thrombin Inhibitors Vitamin K Antagonists Factor Xa Inhibitors (Direct-Acting Oral Anticoagulants) Safety Considerations and Reversal References Anticonvulsant Anticonvulsant Drugs Anticonvulsants Anticonvulsive Drugs Antidepressant Drugs Synonyms Definition Mechanism of Action Clinical Use and Side Effects Cross-References References Antidepressants Antidiuretic Hormone (ADH) Antiepileptic Drugs Synonyms Definition Acetazolamide Mechanism of Action Clinical Use Brivaracetam Mechanism of Action Clinical Use Bromide Mechanism of Action Clinical Use Cannabidiol Mechanism of Action Clinical Use Carbamazepine Mechanism of Action Clinical Use Clobazam Mechanism of Action Clinical Use Clonazepam Mechanism of Action Clinical Use Eslicarbazepine Mechanism of Action Clinical Use Ethosuximide Mechanism of Action Clinical Use Felbamate Mechanism of Action Clinical Use Gabapentin Mechanism of Action Clinical Use Ganaxolone Mechanism of Action Clinical Use Lacosamide Mechanism of Action Clinical Use Lamotrigine Mechanism of Action Clinical Use Levetiracetam Mechanism of Action Clinical Use Oxcarbazepine Mechanism of Action Clinical Use Padsevonil Mechanism of Action Clinical Use Perampanel Mechanism of Action Clinical Use Phenobarbital Mechanism of Action Clinical Use Phenytoin Mechanism of Action Clinical Use Pregabalin Mechanism of Action Clinical Use Primidone Mechanism of Action Clinical Use Rufinamide Mechanism of Action Clinical Use Stiripentol Mechanism of Action Clinical Use Sulthiame Mechanism of Action Clinical Use Tiagabine Mechanism of Action Clinical Use Topiramate Mechanism of Action Clinical Use Valproic Acid (Valproate) Mechanism of Action Clinical Use Vigabatrin Mechanism of Action Clinical Use Zonisamide Mechanism of Action Clinical Use References Antigout Drugs Synonyms Definition Pathophysiology and Clinical Manifestations of Gout Antigout Drugs Mechanism of Action Colchicine Allopurinol Uricosuric Drugs New Drugs Clinical Use (Including Side Effects) Colchicine Allopurinol Uricosuric Drugs Benzbromarone Probenecid Sulfinpyrazone New Drugs Febuxostat Canakinumab References Antihyperglycaemics Antihypertensive Drugs Synonyms Definition Mechanism of Action Angiotensin-Converting Enzyme (ACE) Inhibitors Angiotensin Receptor Blockers (ARBs) Beta-Blockers Calcium Channel Blockers Diuretics Potassium-Sparing Diuretics Additional Antihypertensive Drugs Alpha-Blockers Centrally Acting Sympatholytic Agents Vasodilators Clinical Use References Antihypertensives Anti-integrins Definition of Integrin Anti-integrin Basic Characteristics of Anti-integrins and Mechanisms of Anti-integrin Action Therapeutic Potential of Anti-integrins Specific Anti-integrins Alpha Integrins Alpha 1 Beta 1 Integrin Alpha 2 Beta 1 Integrin (Very Late Activating Antigen 2, VLA2) Alpha 3 Beta 1 Integrin Alpha 4 Beta 1 Integrin (Very Late Activating Antigen 4, VLA4) Alpha 4 Beta 1/Beta 7 Integrin Alpha 5 Beta 1 Integrin Beta 2-Integrin Beta 3 Anti-integrins Alpha IIb/β3 Integrin - Integrin αIIbβ3, Glycoprotein IIb/IIIa (GPIIb/IIIa) Alpha v Beta 3 Integrin Alpha v Beta 6 Integrin Neurotransmitter Receptors and Integrin References Anti-obesity Drugs Synonyms Definition Mechanism of Action Reduction of Energy Intake: Decreasing Fat Absorption Orlistat Reduction of Energy Intake: Decreasing Food Intake Lorcaserin Phentermine/Topiramate Extended Release (ER) Naltrexone Sustained-Release (SR)/Bupropion SR Liraglutide Clinical Use Cross-References References Antioxidants Introduction Definitions: Oxidants, Antioxidants, Free Radicals, ROS Antioxidative Strategies: Endogenous Antioxidants and Pharmacological Approaches Mechanism of Action of Low-Molecular-Mass Antioxidants Endogenous and Exogenous lmm Antioxidants: Two Modes of Action Plant Secondary Metabolites Clinical Use (Incl. Side Effects) References Antiplatelet Drugs Synonyms Definition Mechanism of Action Mechanisms of Platelet Activation Acetylsalicylic Acid (Aspirin) P2Y 12 Receptor Antagonists GPIIb/IIIa (Integrin-IIbβ3) Inhibitors Others Clinical Use References Antiprotozoal Drugs Synonyms Definition Antimalarial Drugs Mechanism of Action Clinical Use Severe Malaria Uncomplicated Malaria Malaria Treatment and Chemoprophylaxis in Nonimmune People Intermittent Preventive Therapy in Pregnant Women and Infants Antimalarial Drugs (P. vivax, P. ovale, P. malariae) Antileishmanial Drugs Mechanism of Action Clinical Use Antitoxoplasma Drugs Mechanism of Action Clinical Use Drugs Against Chagas Disease Mechanism of Action Clinical Use Drugs Against African Sleeping Sickness Mechanism of Action Clinical Use Drugs Against E. Histolytica and G. Lamblia Mechanism of Action Clinical Use References Antiprotozoan Chemotherapeutics Antiseizure Drugs Anti-sense Oligonucleotides Antithyroid Drugs Synonyms Definition Mechanism of Action Pharmacokinetics Clinical Use Side Effects References Anti-TNF Antitussive Drugs Definitions Basic Mechanisms Pharmacological Interventions Drugs Centrally Acting Drugs Opioids Peripherally Acting Drugs Local Anesthetics Cromones GABAB Receptor Agonists Novel Drugs Tachykinin Antagonists (Tachykinins) BW443C Nociceptin/Orphanin Receptor Agonists TRPV1 Receptor Antagonists TRPA1 Receptor Antagonists Potassium Channel Openers Quaternary Ammonium Salts P2x3 Receptor Antagonists References Anxiolysis APEL Apelin Synonyms Definition Basic Characteristic Apelinergic System Apelin in the Cardiovascular System Apelin in Obesity and Diabetes Apelin in Cancer Apelin in Neurodegenerative Diseases Drugs Apelin as a Therapeutic Target Drugs Targeting Apelin/APJ References APJ Endogenous Ligand APLN ApoE Receptors Apolipoprotein E Receptor Family Appetite Control Synonyms Definition Basic Mechanisms Satiety Signals Adiposity Signals Insulin as a Satiety/Adiposity Signal Leptin as an Adiposity Signal Appetite-Regulating Pathways in the Arcuate Nucleus of the Hypothalamus The Melanocortin Signaling System Role of NPY/AGRP Neurons Second-Order Hypothalamic Targets in Adiposity Signaling Other Hormones, Peptides, and Neurotransmitters Involved in Appetite Control Pharmacological Intervention Appetite-Suppressing Drugs Incretin Mimetics Phentermine Bupropion/Naltrexone Lorcaserin Tesofensine Leptin and Leptin Sensitizers Drugs with Appetite-Stimulating Effects Psychotropic Drugs Treatment of Cachexia and Anorexia References Aptamers Definition Basic Mechanisms Aptamer Selection Interactions Between the Target and Aptamer Pharmacological Relevance Aptamers as Diagnostic Agents Aptamer-Fluorophore Conjugates and Optical Sensing Electrochemical Sensing Nanomaterials, Aptamers, and Sensing Aptamers as Therapeutic Agents Functional Therapeutic Designs Using Antidotes Modifications in the Therapeutic Space Aptamers as Drug Delivery Agents Aptamers Conjugated to Small Compounds Aptamer-Oligonucleotide-Based Drug Conjugates Aptamer-Nanoparticle Conjugates Future of Aptamers Challenges to Widespread Use in Clinical Diagnostics Challenges to Widespread Use in Therapeutics References AQP Aquaporins Synonyms Definition Basic Mechanisms Aquaporin Structure-Function Relationships Aquaporin Regulation Aquaporins as Surface Antigens and Cell-Cell Contact Proteins Physiological Functions of Aquaporin Water Permeability Role of Aquaporins in Glycerol Metabolism, Gas Transport, and Redox Signaling Pharmacological Intervention Cross-References References Arginine Vasopressin Argipressin Arteriosclerosis Aryl Hydrocarbon Receptor Definition Basic Characteristics AhR-Mediated Toxicity The AhR Nuclear Translocator: A Partner for the AhR The AhR: Knockout Mice and Cloning AhR: Classical and Non-classical Mechanisms of Action AhR: Role in Multiple Endogenous Functions Drug AhR: Ligand Multiplicity and Selectivity References Assay Development Asthma Asthma Bronchiale Asthma Controllers Atherosclerosis Synonyms Definition Basic Mechanisms Cells Involved in Atherosclerotic Lesions Process of Formation of Foam Cells Recruitment of Circulating Monocytes Foam Cell Formation Macrophage Polarization Inflammatory Responses Macrophage Retention and Emigration Pharmacotherapy for Atherosclerosis Statins (3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase Inhibitor) Fibrates (Peroxisome Proliferator-Activated Receptor-α Agonist) Niacin Cholesterol Absorption Inhibitors ω-3 Polyunsaturated Fatty Acids Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors Antisense Oligonucleotide (ASO) Therapies Microsomal Triacylglyceride Transfer Protein (MTP) Inhibitors ACAT and DGAT Inhibitors References ATP Binding Cassette Proteins ATP Pyrophosphate-Lyase ATP-Dependent K+ Channels Synonyms Definition Basic Characteristics Subtypes Defined by Functional Properties Subtypes Defined by Molecular Cloning The Relationship of Structure to Function Physiology, Pathophysiology, and Therapeutic Potential Insulin Secretion in Pancreatic β Cells Cardiac Function Control of Smooth Muscle Tone Other Roles Drugs Cross-References References ATP-Sensitive Potassium Channels Atrial and Brain Natriuretic Peptides Synonyms Definition Basic Characteristics Characteristics of ANP and BNP Genes and Peptides and Their Regulation of Gene Expression and Secretion Characteristics of Action Drugs ANP and BNP as Diagnostic Agents ANP/BNP System as a Therapeutic Target References Atrial Natriuretic Factor/B-Type Natriuretic Peptide Atypical Antipsychotics Synonyms Definition Mechanism of Action Clinical Use Cross-References References Autoinflammation Autophagy Synonyms Definition Basic Characteristics Autophagy Is Important Outline for a Canonical Autophagic Pathway Networks Regulating Autophagy Drugs Autophagy Activators Versus Inhibitors: Which and When, a Quandary Perspective References B Bacterial Resistance to Antibiotics Introduction Antibiotic Resistance: Definitions Biological Resistance Clinical Resistance Methods for the Determination of Antibiotic Resistance In Vitro Mechanisms of Antibiotic Resistance: Variations of a Theme Genetic Basis of the Transfer of Antibiotic Resistance Molecular Basis of Antibiotic Resistance Mechanisms Alteration of the Target Structure Target Alteration by a Mutation Target Alteration by Producing an Alternate Homologous Target Target Alteration by Enzymatic Modification Reduced Access of the Antibiotic to the Target Structure Reduced Access to the Target due to Reduced Permeability of the Outer Membrane Reduced Access to the Target due to Production of a Target Protecting Protein Reduced Access to the Target due to Production of a Target-Substituting Protein with Reduced Binding Affinity for Antibiotics Enzymatic Inactivation of the Antibiotic Resistance by Enzymatic Hydrolysis of β-Lactam Antibiotics Resistance by Enzymatic Modification of Aminoglycoside-Aminocyclitol Antibiotics Conclusion References Bacterial Toxins Uptake Mechanism of Action Toxins Modifying Target Proteins Bacterial Phospholipases Pore-Forming Toxins Superantigens Clinical Uses Cross-References References Barbiturates Basal Ganglia Base-Excision Repair B-Cell Stimulating Factor 2 Bempedoic Acid Benralizumab Benzodiazepine Definition Mechanism of Action Subtype Specificity of BZ Actions Positive and Negative Allosteric Modulators The Antagonist Flumazenil Pharmacokinetic Considerations Clinical Use References Benzodiazepines Benzoylcholinesterase Beta-Lactam Antibiotics Biocomputing Biologics Biomarkers Bio-originators Biosimilars Blood Glucose-Lowering Drugs Blood Poisoning Blood Pressure Control Synonyms Definition Basic Mechanisms Pharmacological Intervention References Blood Pressure Lowering Drugs Blood Thinners Blood-Brain Barrier Synonyms Definition Basic Mechanisms Cellular Background Endothelial Cells (ECs) Astrocytes Pericytes Microglia Neurons Molecular Background Membrane Transporters Adherens Junctions Tight Junctions Basement Membrane Extracellular Matrix Pharmacological Interventions How to Overcome the BBB? References Blood-Brain Interface Blood-Testis Barrier Synonyms Definition Basic Mechanisms Background Ultrastructural Features of the Blood-Testis Barrier (BTB) Pharmacological Intervention Regulatory Bioactive Peptides of the BTB Summary Cross-References Acknowledgments References Blood-Tissue Barrier in Testes BMH1 BMH2 Bone Metabolism Synonyms Definition Basic Mechanisms Biochemical Composition of Bone Bone Structure Mechanisms of Bone Remodeling Hormonal Regulation of Mineral Homeostasis and Bone Remodeling Pharmacological Intervention References Bone Morphogenetic Proteins Introduction Basic Characteristics BMP Signalling Crosstalk BMP Pharmacology Future Directions Acknowledgments References Bone Remodeling Bone Turnover Bortezomib (Velcade) Botulinum Neurotoxins Definition, Serotypes, and Subtypes Botulism and Botulinum Neurotoxins Basic Mechanism of Nerve Terminal Paralysis by the Botulinum Neurotoxins Neurospecific Binding Internalization into Nerve Terminals Membrane Translocation Reduction of the Disulfide Interchain Bond SNARE Protein Cleavage Duration of the Peripheral Neuroparalysis Induced by Botulinum Neurotoxins Long-Distance Effects of Botulinum Neurotoxins Clinical Use BoNT Formulations Therapeutic Applications Adverse Effects Acknowledgments References Bradykinin Brain Capillary Endothelial Cells Bremelanotide Synonyms Definition Mechanism of Action Clinical Use (Including Side Effects) Phase 1 Clinical Trials Phase 2 Clinical Trials Phase 3 Clinical Trials References Bromodomain Inhibitors Bronchial Asthma Synonyms Definition Basic Mechanisms Cardinal Symptoms Early and Late Phase in Allergic Asthma Inflammation Hyperresponsiveness Bronchial Remodeling (BHR) Drug-Sensitive Asthma General Principles of Managing Asthma Pharmacological Interventions Allergen-Specific Immunotherapy (SIT) β2-Receptor Agonists Anticholinergics Anti-leukotriene Therapy Corticosteroids (CS) Biologicals Anti-IgE Antibodies Against IL-4, IL-5, and IL-13 Rarely Used Therapeutics Future Therapeutic Options References Butyrylcholinesterase (EC 3.1.1.8) (BChE or BuChE): ChE C C Kinase Ca2+ Antagonists Ca2+ Channel Antagonists Ca2+ Channel Blockers Synonyms Definition Mechanism of Action Ca2+ Channel Physiology Ca2+ Channel Function Ca2+ Channel Types L-Type Ca2+ Channel Blockers Dihydropyridines (DHPs) Phenylalkylamines Benzothiazepines Clinical Use (Including Side Effects) Side Effects Other Pharmacological Actions of Ca2+ Antagonists Cross-References References Ca2+-Binding Proteins Synonyms Definition Basic Characteristics and Clinical Relevance Cardiology Oncology Inflammation and Allergies Brain Injury and Neuropathology Drugs Outlook References Ca2+-Induced Ca2+ Release (CICR) Channel Ca2+-Sensing Receptor (CaSR) Synonyms Definition Basic Characteristics Drugs References Cadherins/Catenins Synonyms Definition Basic Characteristics Structural Characteristics of Cadherins Cytoplasmic Interactions of Cadherins Gene Organization Functional Characteristics β-Catenin in the Wnt Pathway Drugs References Calcidiol Calciol Calcitonin Family Receptors Synonyms Definitions Basic Characteristics Peptides Receptors - Overview Receptor Composition and Pharmacology Molecular Understanding of Receptor Pharmacology Physiological Relevance of These Receptors Drugs CT-Based Drugs and Diagnostics Amylin-Based Drugs CGRP-Based Drugs AM-Based Drugs and Diagnostics Cross-References References Calcitriol Calcium-Binding Calcium-Dependent Adhesion Protein/Plakoglobin Calcium-Sensing Receptor Canakinumab Cancer Cancer Immunotherapy Synonyms Definition Basic Mechanism Monoclonal Antibodies Immune Checkpoint Inhibitors Cellular Immunotherapy Vaccines Others Pharmacological Relevance (Including Side Effects) Cross-References References Cardiac Arrest Cardiac Glycosides Synonyms Mechanism of Action Clinical Use Cross-References References Cardiac Infarction Cardiac Steroids Cardiomyopathy Cardiotonic Steroids Carfilzomib (Kyprolis) Catechol-O-Methyltransferase Synonyms Definition Mechanism of Action COMT Inhibitors Clinical Use (Including Adverse Effects) Cross-References References Cell Cycle Checkpoints Cell Cycle Regulation Definition Basic Mechanisms Cell Cycle Regulation by Protein Phosphorylation Cell Cycle Regulation by Ubiquitin-Mediated Protein Degradation G1/S Transition and Transcriptional Control Cell Cycle Control by CDK Inhibitors Cell Cycle Checkpoints DNA Damage and Replication Checkpoint Spindle Assembly Checkpoint Pharmacological Intervention to the Cell Cycle Pharmacological CDK Inhibitors Pharmacological Cell Cycle Inhibitors Pharmacological Abrogation of Cell Cycle Checkpoints References Cellular Senescence Cephalosporins Synonyms Definition Chemistry Mechanism of Action Clinical Use (Including Side Effects) References Cerebral Microvessels CGRP Receptor Chaperones Synonyms Definition Basic Mechanisms Molecular Chaperones RNA Chaperones Chaperone Diseases Pharmacological Intervention Chemical Chaperones Drugs That Target Molecular Chaperones References ChE ChE I ChE II Checkpoint Inhibitors (CPI) Chemical Biology Chemical Probes Chemoattractant Receptors Chemokine Receptors Synonyms Definition Basic Characteristics Chemokine Receptors Role in Immune Response Drugs Chemokine Receptors in Pathogen Infection References Chemokines Chloride Channels Cholesterol Oxidation Products Cholesteryl Ester Transfer Protein Inhibitors Cholinesterases Synonyms Definition Basic Characteristics Cellular Processes Catalytic Activity Non-catalytic Activity Structure Molecular Mechanisms of Assembly Genetics and Evolution Posttranscriptional Modifications Posttranslational Modifications Molecular Forms of ChEs Drugs Cholinesterase Inhibitors Drugs Chemical Warfare Agents, Pesticides, and Insecticides References Chromatin Remodeling Chronic Bronchitis Chronic Obstructive Pulmonary Disease Synonyms Definition Basic Mechanisms Pharmacological Interventions Bronchodilators Anti-inflammatory Therapy Anti-microbial Therapy Anti-trypsin Augmentation Therapy Oxygen Therapy Psychopharmacological Therapy Non-pharmacological Interventions (Singh et al. 2019) Reduction of Risk Factors Vaccination Noninvasive Ventilation Pulmonary Rehabilitation Lung Volume Reduction (Surgery and Endoscopic) References Circadian Rhythms Synonyms Definition Basic Mechanisms The Circadian Timing System Circadian Rhythms of Key Intracellular Pathways Circadian Rhythms of Physiological Functions Governing Drug Absorption, Distribution, Metabolism, and Excretion (ADME) Inter-Individual Variabilities in Circadian Rhythms Clock Disruption and Pathologies Pharmacological Intervention Intervention to Restore Normal CTS Functions Chronotherapies of Selected Pathologies Rheumatology Cardiovascular Pathologies Anticancer Chronotherapies Cross-References References Cl- Channels and Cl-/H+ Exchangers Synonyms Definition Basic Characteristics Classification of Chloride Channels Gene Families of Chloride Channels The CLC Family of Chloride Channels and Transporters in Mammals TMEM16/ANO Ca2+-activated Chloride Channels CFTR Bestrophins LRRC8/VRACs: Volume-Regulated Anion Channels TMEM206/ASOR Acid Activated Anion Channels Drugs References Classic Hallucinogen Clinical Chemistry CNP COMT COMTase Connexin Hemichannels Synonyms Definition Basic Characteristics Life Cycle Regulation Drugs Peptides Targeting the Connexin Extracellular Loop Peptides Targeting the Connexin Cytoplasmic Loop References Consumption Contraceptives Synonyms Definition Mechanism of Action Clinical Use (Including Side Effects) Cross-References References Control of Food Intake Control of Hypertension Corticosteroids Corticotropin-Releasing Factor (CRF) System Corticotropin-Releasing Hormone System Synonyms Definition Basic Characteristics CRH and Its Related Neuropeptides Members of the CRH-Related Neuropeptide Family Expression Pattern CRH-Binding Protein CRH Receptors Splice Variants Expression Pattern Receptor Interactions Ligand-Receptor Interaction Receptor-Receptor Interaction CRH-Dependent Signaling The CRH System and Its Connection to Stress Hypothalamic-Pituitary-Adrenal Axis Behavioral Stress Responses Therapeutic Potential of the CRH System in Stress-Related Disorders Drugs References COX CTLA8 C-Type Natriuretic Peptide and Its Receptors Synonyms Definition Basic Characteristics C-Type Natriuretic Peptides C-Type Natriuretic Peptide Receptors and Enzymes Sites of Expression and Biological Roles Measurement of C-Type Natriuretic Peptides in Human Plasma Drugs CNP Analogs Other Ligands of CNP Receptors Inhibition of Neprilysin Cross-References References Cyclic AMP-Dependent Protein Kinase Anchoring Proteins Cyclin-Dependent Kinase Inhibitors Cyclin-Dependent Kinases as Therapeutic Targets Synonyms Definition Inhibitors of Cell Cycle CDKs Inhibitors of Non-Cell Cycle CDKs Modes of CDK Inhibition Revelations from the Clinical Use of CDK4/6 Inhibitors References Cyclizing (E.C.4.6.1.1.) Cyclooxygenases Synonyms Definition Basic Characteristics Structural Features Reaction Mechanisms Roles in Physiology and in Pathophysiology Drugs Conclusions and Future Perspectives of COX Inhibitors Cross-References References Cytochrome P450 (CYP) Cytochrome P450 Isozymes Cytochrome P450 Monooxygenases Cytokines Synonyms Definition Basic Characteristics Mechanism of Action Cytokines and Therapy Clinical Use (Including Side Effects) Examples of Recombinant Cytokines Currently in Use Interferons Inhibitors of Cytokine Action Cross-References References Cytoplasmic Tyrosine Kinases D Daily Rhythms Dalteparin Dementia due to Alzheimer´s Disease Depressive Illness Derivatives of the 7-Aminocephalosporanic Acid DesArg10-Kallidin (Lys0, desArg9-Bradykinin) DesArg9-Bradykinin Deubiquitinases Deubiquitylating Enzymes Synonyms Definition Basic Characteristics Characteristics of Ubiquitylation Characteristics of Deubiquitylating Enzymes DUBs in Cellular Signaling Regulation of p53 Signaling Regulation of NF-κB Signaling Regulation of TGF-β Pathway Cytokine-Inducible Deubiquitinating Enzymes DUBs as Clinical Markers of Cancers DUBs in Immunity and Inflammation DUBs in Infectious Diseases Drugs References Diabetes Mellitus Definition Basic Mechanisms Type 1 Diabetes (Previously Insulin-Dependent Diabetes Mellitus, IDDM, or Juvenile Diabetes) Type 2 Diabetes (Previously Non-Insulin-Dependent Diabetes Mellitus, NIDDM) Pharmacological Intervention References Diabetes-Associated Peptide Diagnostics Differentiation Factors Digitalis Disease-Modifying Anti-rheumatic Drugs DNA Damage Response Synonyms Definition Basic Mechanisms Pharmacological Intervention Targeting the DNA Damage Response Single-Agent Strategies Targeting DNA Damage Sensor Proteins PARP Inhibitors Current Licensed PARP Inhibitor Indications Ovarian Cancer Maintenance Setting Upfront Setting Recurrent Setting Beyond Ovarian Cancer Breast Cancer Emerging Monotherapy Indications Beyond Monotherapy Approaches Combination Strategies Combinations with Other DDR Pathway Inhibitors Combinations with Immune Checkpoint Blockade Conclusion References DNA Gyrase Inhibitors Synonyms Definition DNA Gyrase Inhibitors Mechanism of DNA Supercoiling by DNA Gyrase Mechanism of Action of DNA Gyrase Inhibitors Clinical Use References DNA Methylation DNA Topoisomerase II Inhibitors Docking Protein Dopamine Dopamine System Synonyms Definition Basic Characteristics Dopaminergic Pathways Dopamine Dopamine Synthesis Dopaminergic Receptors Dopaminergic Signaling Disorders Associated with Dopaminergic System Dopaminergic Drugs References Dopaminergic Receptors Drug Discovery Drug Interactions Synonyms Background Clinical Significance of Drug-Drug Interactions Basic Mechanisms Pharmacodynamic Interactions Pharmacodynamic Interactions as Cause of Bleeding Events Pharmacokinetic Interactions Regulatory Requirements DDI on the Level of Adsorption Interactions on the Level of Drug Transporters Pharmacokinetic Interactions on the Level of Metabolism Induction of Transport and Metabolism Conclusions References Drug Receptor Theory Drug Screening Drug Targets Drug-Drug Interactions Drug-Receptor Interaction Synonyms Definition Basic Mechanisms Pharmacological Relevance Cross-References References Drugs for the Treatment/Management of Gout and/or Hyperuricemia E Early Drug Discovery EC 2.1.1.6 EF-Hand EFNA1, EphrinA1, Ephrin-A1 EFNA2, EphrinA2, Ephrin-A2 EFNA3, EphrinA3, Ephrin-A3 EFNA4, EphrinA4, Ephrin-A4 EFNA5, EphrinA5, Ephrin-A5 EFNB1, EphrinB1, Ephrin-B1 EFNB2, EphrinB2, Ephrin-B2 EFNB3, EphrinB3, Ephrin-B3 Eicosanoids Emesis Definitions Basic Mechanisms Vomiting Nausea Pharmacological Interventions Muscarinic Receptor Antagonists (Sanger and Andrews 2018) Histamine H1 Receptor Antagonists (Sanger and Andrews 2018) Dopamine D2 Receptor Antagonists (Sanger and Andrews 2018) 5-Hydroxytryptamine3 (5-HT3) Receptor Antagonists (Sanger and Andrews 2018) Neurokinin1 (NK1) Receptor Antagonists (Sanger and Andrews 2018) Treating Nausea: A Remaining Challenge Genomics and Emesis References Endocannabinoids Synonyms Definition Basic Characteristics Endocannabinoid Biosynthesis Endocannabinoid Action Endocannabinoid Inactivation Endocannabinoid Membrane Transport The Endocannabinoidome Drugs Pathological Conditions in Which Endocannabinoids Are Involved Endocannabinoid-Based Drugs Cross-References References Endogenous Agonists of Cannabinoid Receptors Endoplasmic Reticulum Stress Endothelins Definition Basic Characteristics Endothelin and Endothelin-Converting Enzymes Endothelin Receptors Sites of Endothelin Receptor Expression Genetic Studies and Human Diseases Drugs Clinical Use References Enoxaparin Eosinophils Eph Receptors and Ephrins Synonyms Definition Basic Characteristics Domain Structure Signal Transduction Eph Receptor Signaling Ephrin Signaling Cellular Effects of Eph Receptor/Ephrin Signaling Physiological and Pathological Functions Nervous System Epithelia Cardiovascular and Lymphatic Systems Immune System Other Functions Diseases Cancer Neurodegeneration Parasitic Infections Drugs Cross-References References EPHA1 EPHA10 EPHA2 EPHA3 EPHA4 EPHA5 EPHA6 EPHA7 EPHA8 EPHB1 EPHB2 EPHB3 EPHB4 EPHB6 EPHX2 Epigenetic Therapy Epigenetics Synonyms Definitions Basic Mechanisms DNA Methylation Histone Acetylation Bromodomain-Containing Proteins Recognize Acetylated Histone Histone Methylation Pharmacological Intervention Targeting DNA Methylation Targeting Histone Acetylation Targeting Histone Methylation Targeting Epigenetic Readers References Epithelial Na+ Channel Definition Basic Characteristics Channel Family and Structural Organization Physiological Roles Mechanisms of ENaC Regulation Drugs References EPO, Recombinant Erythropoietin, Epoetin and Darbepoetin Alfa Epoxide Hydrolase 2 Erythrocyte ChE Extracellular Matrix (ECM) Definition Basic Characteristics Characteristics of the Extracellular Matrix (ECM) The ECM in Disease Drugs Targeting the ECM Gene Therapy Direct Targeting of the ECM and Downstream Cellular Effectors Future Considerations in Drug Development Final Thoughts References F Ferroptosis Lipid Peroxidation of Membranes in Ferroptosis Iron and Ferroptosis Scavenging and Detoxification of Lipid Peroxides Ferroptosis and Disorders Summary References Fever Definition Basic Mechanisms Exogenous and Endogenous Pyrogens Actions of Pyrogens (PGE2) on the Thermoregulatory System Transfer of Fever-Generating Signals Across the Blood-Brain Barrier Sensory Circumventricular Organs (CVOs) Cells Forming the Blood-Brain Barrier (BBB) Transport of Pyrogens Across the Blood-Brain Barrier Inflammatory Signal Transfer from the Periphery to the Brain Via Sensory Nerves Pharmacological Intervention References Fibrates Fibroblast Growth Factors Definition Basic Characteristics FGFs FGFRs and HSPGs FGF/FGFR Signaling FGFs in Physiology Embryonic Development Tissue Homeostasis Wound Healing FGFs in Pathology Genetic Diseases Cancer Other FGF-Related Pathologies Drugs References Fondaparinux Foot Fragment-Based Drug Discovery Free Fatty Acid Receptors Definition Basic Characteristics FFA1 FFA2 and FFA3 FFA4 Drugs and Pharmacological Relevance References G GABAergic System Synonyms Definition Basic Characteristics Drugs Benzodiazepines Barbiturates General Anesthetics Neurosteroids GABAA Receptor Mutants as Models for Disease References Gap Junction Hemichannels Gastric Motility Gene Expression Analysis and Next-Generation Sequencing Synonyms Definition Description Pharmacological Relevance References Gene Expression Profiling Gene Medicine Gene Therapy Gene Therapy Vectors Synonyms Definition Description Design of Viral Vectors Types of Viral Vectors Adenoviruses Adeno-associated viruses (AAV) Retroviral Vectors Delivery, Tropism, and Targeting Regulation of Gene Expression Other Viral Vectors Potential Risks Pharmacological Relevance Cross-References References Gene Transfer General Anesthetics Genetics Ghrelin Ghrelin, Physiological Roles and Clinical Relevance of Synonyms Definition Basic Mechanism Ghrelin Production and Acylation The Ghrelin Receptor and Its Signaling Pathways Role of Ghrelin in the Regulation of Growth Hormone Role of Ghrelin in the Homeostatic Regulation of Appetite Role of Ghrelin in the Hedonic Regulation of Appetite Role of Ghrelin in Stress and Anxiety Role of Ghrelin in Memory and Neuroprotection Effects of Ghrelin on the Autonomic Nervous System The Current Understanding of the Spatial Separation Between Ghrelin and the GhrR in the Brain Role of Ghrelin in Gastric Motility Role of Ghrelin in Glucose Metabolism Pharmacological Intervention Clinical Findings of Ghrelin´s Effect on Growth Hormone Clinical Findings of Ghrelin´s Effect on Appetite and Body Weight Clinical Findings of Ghrelin´s Effect on Anxiety and Alcohol Dependence Clinical Findings of Ghrelin´s Effect on Neuroprotection Clinical Findings of Ghrelin´s Effect on the Autonomic Nervous System Clinical Findings of Ghrelin´s Effect on Gastric Motility Clinical Findings of Ghrelin´s Effect on Glucose Metabolism GhrR Antagonism Cross-References References GhrR Glucocorticoid Agonists Glucocorticoids Synonyms Definition Regulation of Inflammation Mechanism of Gene Induction by NF-κB Mechanisms of Glucocorticoid Functions Gene Induction Inflammatory Gene Suppression by Glucocorticoids Other Mechanisms of GR Regulation of Inflammation Nongenomic Actions of Glucocorticoids Clinical Use (Including Side Effects) Combination Therapy in Asthma Glucocorticoid-Induced Adverse Effects Approaches for Reducing Glucocorticoid-Induced Side Effects Cross-References References Glucose Metabolism Glucose-Lowering Drugs Other than Insulin Synonyms Definition Mechanism of Action Biguanide Sulphonylureas Prandial Insulin Releasers (Meglitinides) Dipeptidyl Peptidase-4 Inhibitors Glucagon-like Peptide-1 Receptor Agonists Sodium-Glucose Cotransporter-2 Inhibitors Thiazolidinediones α-Glucosidase Inhibitors Pramlintide Bromocriptine Colesevelam Clinical Use Cross-References References Glycine Receptors Synonyms Definition Basic Characteristics Glycinergic Synapses Excitatory Role of GlyRs in Immature Neurons Glycine Receptor Structure-Function Relationship Interaction of GlyRs with Intracellular Proteins Physiological Consequences of Impaired Glycinergic Function Allosteric Pharmacological Modulation References Glycine-Gated Chloride Channel GPCR GPR4 G-Protein-Coupled Receptors Definition Basic Characteristics Structure and Function Classification Dimerization Physiological Functions Pharmacological Modulation Drugs Cross-References References Gram-Negative Bacteria Granulocyte Colony-Stimulating Factor (G-CSF), Filgrastim, Pegfilgrastim and Lenograstim Granulocyte Macrophage Colony-Stimulating Factor (GM-CSF), Molgramostim and Sargramostim Growth Factors Synonyms Definition Historical Perspective Concerted Actions of Growth Factors: Wound Healing as an Example Growth Factor Families Biochemical Mechanisms Activated by Growth Factors Drugs Targeting Growth Factors and Downstream Signaling Pathways Cross-References References Growth Hormone Guanyl Cyclase Guanylate Cyclase Guanylyl Cyclase Synonyms Definition Basic Characteristics NO-Sensitive GCs Transmembrane GCs Drugs Drugs Acting on NO-Sensitive GCs NO-Releasing Compounds NO-GC Sensitizers and NO-Heme-Mimetics (~ciguat) Drugs Acting on Receptor-Linked GCs GC-A Ligands Elevating Natriuretic Peptides GC-C Ligands Cross-References References H Hallucinogen HCN Channels Definition Basic Characteristics Drugs References Head Injury Heart Attack Heart Failure Synonyms Definition Basic Mechanisms Heart Failure with Reduced Ejection Fraction Heart Failure with Preserved or Mid-Range Ejection Fraction Neuroendocrine Activation Natriuretic Peptides Pharmacological Intervention Diuretics Beta Blockers (BB) ACE Inhibitors Angiotensin Receptor Blockers (ARB) Angiotensin and Neprilysin Inhibitors Mineralocorticoid Receptor Antagonists Ivabradine Additional Drugs Conclusion References Heat Shock Proteins (Hsp) Hedonic Appetite Hematopoietic Growth Factors Synonyms Definition Erythropoietin (EPO) Mechanism of Action Clinical Use Granulocyte Colony-Stimulating Factor (G-CSF) and Granulocyte Macrophage Colony-Stimulating Factor (GM-CSF) Mechanism of Action Clinical Use Interleukin-11 (IL-11) Mechanism of Action Clinical Use References Heparin and Related Drugs Synonyms Definition Structure and Origin Mechanism of Action Additional Anticoagulant Mechanisms of Action Low Molecular Weight Heparins: Mechanisms of Action Units of Activity of Heparin Clinical Uses of Heparin Heparin Clearance from the Circulation Heparin Neutralizing Agents Non-bleeding Side Effects of Heparin Treatment Heparin Contamination Other Heparin-Protein Interactions Cross-References References Hepatocyte Stimulating Factor Heterodimerization HGFs High Content Screening High Voltage-Activated (HVA) Calcium Channels High-Throughput Screening High-Throughput Screening (HTS) High-Throughput Screening (HTS) Technology Synonyms Definition Description Assay Detection Technologies Data Analysis Pharmacological Relevance References Hippo Pathway Definition Basic Characteristics Hippo Pathway Activation-Inactivation Hippo Kinase Cassette YAP/TAZ TEAD Genetic Dysregulation of the Hippo Pathway Pathophysiology and Therapeutic Potential Pharmacological Intervention References Histamine Receptors Synonyms Definition Basic Characteristics Classification Expression and Function H1 Receptor H2 Receptor H3 Receptor H4 Receptor Structure and Signaling H1 Receptor H2 Receptor H3 Receptor H4 Receptor Drugs H1 Receptor Ligands H2 Receptor Ligands H3 Receptor Ligands H4 Receptor Ligands References Histaminergic Receptors Histone Acetylation Histone Deacetylases Histone Methylation Homeostatic Appetite Homologous Recombination Deficiency Hormonal Contraceptives Hormonal Regulation of Transcription Hybridoma-Plasmacytoma Growth Factor, 26 kDa Protein Hydroxyaryl-Protein Kinase 5-Hydroxytryptamine = 5-HT (= Enteramine) Hypoglycaemic Agents I IL-1 IL-17 IL-17A IL-1R IL-23 IL23A IL-23p19 IL-5 Immune Checkpoint Blockade Synonyms Definition Basic Mechanism Mechanism of Action Biomarkers Mechanisms of Resistance Pharmacological Relevance Side Effects Cross-References References Immune Checkpoint Inhibitors Immune Treatment Immuno-oncology Immunoresolvents Immunotherapy Infection Inflammasome Definition Role of Inflammasomes in Infection and Diseases Mechanisms of NLRP3 Inflammasome Activation Therapies Targeting the NLRP3 Inflammasome References Inflammation Definition Basic Mechanisms Introduction Cells and Mediators of Acute Inflammation The Endothelial Cell The Neutrophil The Monocyte/Macrophage Mediators of Inflammation Healing Chronic Inflammation Cross-References References Inhibitors Inhibitory Glycine Receptor Inhibitory Neurotransmission INSL3 INSL5 INSR (Gene Name) Insulin Receptor Synonyms Definition Basic Characteristics Structure and Function Signal Transduction and Insulin Action Drugs Agents Stimulating the Receptor or the Signaling Pathway Agents Inhibiting Insulin Receptor Signaling References Insulin Secretagogues Integrins as Drug Targets: Is There a Future? Background Thrombosis Signaling Cancer Infection and Immunity Conclusion References Interferons Interleukin 11 (IL-11) Interleukin-1 (IL-1) Synonyms Definition Basic Characteristics The IL-1 Receptor Overlapping and Distinct Features of IL-1α and IL-1β Endogenous Regulators of IL-1 Activity IL-1 in Human Disease Drugs References Interleukin-17 Synonyms Definition Basic Characteristics IL-17 Cytokine and Receptor Family IL-17 Signaling Cellular Sources of IL-17 IL-17 Roles in Health and Disease IL-17 in Autoimmune Disease Psoriasis Spondyloarthritides and Other Diseases Drugs Cross-References References Interleukin-23 Synonyms Definition Basic Characteristics IL-23 Discovery and Signaling Expression of IL-23 and IL-23R Biological Consequences of IL-23 Signaling in Health Biological Consequences of IL-23 Signaling in Autoimmune Diseases Other Biological Consequences of IL-23 Signaling Therapeutic Agents Targeting IL-23 Cross-References References Interleukin-5 Synonyms Introduction Background The Axis of IL-5 and IL-5R Eosinophils and Disease Therapeutic Interventions with IL-5 Antagonism Mepolizumab Reslizumab Benralizumab Conclusions Acknowledgment References Interleukin-6 Synonyms Definition Basic Characteristics Molecular Tools to Study Interleukin-6 Pharmacological Relevance Pathophysiological and Therapeutic Relevance Outlook References Interleukins Inward Rectifier Potassium Channels Synonyms Definitions Molecular Basis and Functional Diversity of Kir Channels Molecular Structure of Kir Channels The Mechanism of Strong Inward Rectification Structural Elements of Inward Rectification Pharmacology of Kir Channels Diseases Resulting from Kir Channel Mutations References Inward Rectifiers Inwardly Rectifying Potassium Channels Islet Amyloid Polypeptide Ixazomib (Ninlaro) J JAK Inhibitors JAK-STAT Pathway Definition Basic Characteristics Physiological Functions of JAKs Roles of STAT Proteins in Gene Induction Drugs References Janus Kinase Synonyms Definition Basic Characteristics Janus Kinases and the Cytokine Signaling Function and Regulation of JAKs Downstream Signaling Intramolecular Regulation of JAK Kinases Intermolecular Regulation of JAK Kinases JAK-STAT Signaling in Disease Drugs Approved JAKinibs Ruxolitinib Tofacitinib Baricitinib Fedratinib Upadacitinib Peficitinib JAKinibs in Clinical Trials JAK1-Selective Inhibitors JAK2-Selective Inhibitors JAK3-Selective Inhibitors TYK2-Selective Inhibitors References Just Another Kinase K Kallidin (Lysyl-Bradykinin) Kinins Synonyms Definition Basic Characteristics Liberation of Kinins Bradykinin Diagnostics of Kinins Kinin Receptors Kinin Receptor-Deficient Mice Biological Functions and Clinical Implications Drugs References Kir Channels Kv-Channels L Laboratory Medicine Lactam β Antibiotics β-Lactam Antibiotics Synonyms Definition Mechanism of Action Lethal Target Proteins β-Lactamase-Mediated Resistance PBP-Mediated Resistance Outer Membrane Permeability and Active Efflux Systems Clinical Use References L-DOPA Lead Discovery by NMR LEAP2 Leonardo 8-Leucine-Vasotocin Leukotrienes Synonyms Definition Basic Mechanisms Pharmacological Relevance Production of LTB4 Metabolism of LTB4 Characteristics of LTB4 Receptors LTB4 in Health and Diseases Characteristics of Cys-LTs Production of Cys-LTs Metabolism of LTE4 Characteristics of Cys-LT Receptors Other Receptors for Cys-LTs Cys-LTs in Health and Diseases References Lipid Mediators Lipid-Lowering Drugs Synonyms Definition and Introduction Mechanisms of Action and Clinical Use LDL-C, Non-HDL-C, and ApoB Lowering Drugs in Current Use Statins PCSK9 Inhibitors Inhibitors of Intestinal Cholesterol Absorption Bile Acid Sequestering Agents Inhibitors of ApoB Synthesis Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) Triglyceride-Lowering Drugs in Current Use Fibrates Omega-3 Fatty Acids Niacin Lipid-Lowering Drugs Not Currently Used Clinically Inhibitors of Cholesteryl Ester Transfer Protein (CETP) Inhibition of Adenosine Triphosphate Citrate Lyase with Bempedoic Acid Inhibitors of Lipoprotein (a) (Lp(a)) Synthesis Inhibitors of ApoC-III Synthesis References Lipoprotein Receptors Local Anesthetic Drugs Local Anesthetics Synonyms Definition Mechanism of Action Chemistry Sodium Channel Blockade Clinical Use Cross-References References Low Molecular Mass GTPases Low Molecular Weight Heparin (LMWH) Low Voltage-Activated (LVA) Calcium Channels Low-Density Lipoprotein Receptor Gene Family Synonyms Definition Basic Characteristics Structural Organization of the LDL Receptor Gene Family Receptor-Mediated Endocytosis and Signal Transduction Functions of LDL Receptor Gene Family Members LDL Receptor LRP1 VLDLR and APOER2 (LRP8) LRP4 LRP5 and 6 LRP1B LRP2 Drugs Statins PCSK9 Inhibitors Romosozumab Lipoprotein Receptors for Drug Delivery References Low-Density Lipoprotein Receptor-Related Proteins LRP Lymphokines Lysoglycerophospholipids Lysolipid Mediators Lysophosphatidic Acid Definition Basic Characteristics Metabolism LPA Receptors Biological Actions Drugs References Lysophospholipids Synonyms Definition References Lysosphingolipids M Macroautophagy MAP Kinase Cascades Synonyms Definitions Basic Characteristics Characteristics of MAPK Cascades Characteristics of the ERK1/2 Pathway Characteristics of the ERK5 Pathway Characteristics of the JNK Pathway Characteristics of the p38 Kinase Pathway Drugs References Matrix Metalloproteinases Synonyms Definition Basic Characteristics Drugs References Mechanistic/Mammalian Target of Rapamycin Complex 1 Signaling Network Melatonin Synonyms Definition Basic Characteristics Melatonin Receptor Types Physiology Aging Sleep and Circadian Rhythms Metabolic Regulation Non-receptor-Mediated Properties: Antioxidant and Anti-Inflammatory Effects Pathophysiology Neuropsychiatric Disorders Type 2 Diabetes Mellitus and Obesity Drugs References Mepolizumab 5-Methoxy-N-Acetyltryptamine Microsomal Triglyceride Transfer Protein Inhibition Misfolded Proteins Mitochondrial Selective Autophagy Mitogens Mitophagy Synonyms Definition Basic Characteristics Molecular Mechanisms of Mitophagy The PINK1/Parkin Pathway Receptor-Mediated Mitophagy Basal, Stress-Induced, and Programmed Mitophagy Drugs General Mitochondrial Targeting Agents to Manipulate Mitochondrial Turnover Maintenance of Mitochondrial Homeostasis Through the Regulation of NAD+ Metabolism Natural Chemical Agents with Mitophagic Capacities Mitophagy Inhibitors References Mixed-Function Oxidases MMPs Molecular Chaperones Molecular Dynamics Molecular Modelling Synonyms Definition Description Sequence Similarity Protein Structure Predictions Homology Models of Protein Structures Molecular Simulation Docking Accuracy and Limitations Pharmacological Relevance Structure-Function Prediction Simulation of Functional Properties References Molecular Simulation Monoamine Oxidases Monoamine Oxidases and Their Inhibitors Synonyms Definition Reaction Mechanism of Monoamine Oxidase Basic Characteristics of Monoamine Oxidases Drugs Neuropharmacology of Monoamine Oxidases and Their Inhibitors The Cheese Reaction Monoamine Oxidase Inhibitors as Therapeutic Agents Parkinson´s Disease Neuroprotection in Neurodegenerative Diseases Depressive Illness Reading List Monokines Mood Elevators Mood Stabilizers Definition Mechanism of Action Clinical Use, Efficacy, and Side Effects Lithium Valproate Lamotrigine Quetiapine Other Treatment Options Acknowledgments References Morbus Alzheimer MS MSU mTOR Signaling Pathways Synonyms Definition Basic Characteristics Upstream of mTORCs Downstream of mTORCs Drugs Rapamycin and ``First Generation´´ mTOR Inhibitors Dual PI3K/mTOR Inhibitors Second-Generation mTOR Inhibitors Third Generation of mTOR Inhibitors mTOR Complex-Specific Inhibitors References Multidrug-Resistant Multiple Sclerosis Synonyms Definition Basic Mechanisms Pharmacological Intervention/Pharmacotherapy Parenteral Drugs Oral Drugs Future Directions References Muscarinic Acetylcholine Receptors Muscarinic Receptors Synonyms Definition Basic Characteristics General Structural Features Distribution and Physiological Functions of mAChRs Ligands and Mechanisms Involved in Ligand Binding and mAChR Activation Allosteric Modulators of mAChR Function G Protein-Coupling Properties of mAChRs Signaling Pathways Activated by mAChR Subtypes Regulation of mAChR Activity Drugs Current Clinical Uses of Muscarinic Drugs Potential Clinical Uses of Muscarinic Drugs References Myocardial Infarct Myocardial Infarction Synonyms Definition Pathophysiologic Mechanisms General Coronary Artery Disease Stable Coronary Plaques Vulnerable Coronary Plaques Acute Coronary Syndrome Electrocardiogram Cardiac Biomarkers Myocardial Cell Death Reperfusion Injury Type II Myocardial Infarction Pharmacological Intervention Fibrinolysis Antiplatelet Agents Anticoagulant Agents Secondary Prevention Cross-References References Myorelaxation N Na +/K +-ATPase: Na +/K + Exchanging ATPase Na+/Ca2+ Antiporter Na+/Ca2+ Exchanger Na+/Ca2+ Exchangers Synonyms Definition Basic Characteristics Molecular Biology and Topology Distribution Regulatory Factors Transcriptional Factors Regulating NCX Expression Physiological Roles Pathophysiological Implications Drugs Molecular Pharmacology of Na+/Ca2+ Exchanger Glossary References Na+/H+ Exchangers Synonyms Definition Basic Characteristics SLC9A Subfamily SLC9B Subfamily SLC9C Subfamily Drugs References Na+/K+-ATPase Synonyms Definition Basic Characteristics The Subunit Composition of Na+/K+-ATPase Na+/K+-ATPase Acts as a Sodium-Potassium Pump Drugs The Na+/K+-ATPase Is the Molecular Target for Cardiotonic Steroids (CTS) and Palytoxin Na+/K+-ATPase Acts as Signal Transducer for Cardiac Glycosides Endogenous Cardiac Glycosides Act as Hormones Rostafuroxin, A Cardenolide Derivative with Antihypertensive Action Natural and Synthetic Cardenolides and Bufadienolides as Anti-Cancer Agents References N-Acetyl-5-Methoxytryptamine NAD(P)H Oxidase NAD(P)H:Oxygen Oxidoreductase NADPH Oxidase Synonyms Definition Basic Characteristics Prototype NADPH Oxidase Isoforms Biological Functions Drugs References NCX NCX1 NCX2 NCX3 Neprilysin Inhibitors Neprilysin and the Natriuretic Peptides Neprilysin Inhibitors ARNIs in HFrEF and HFpEF References Neurodegeneration Synonyms Definition Basic Mechanisms Necrosis Apoptosis Regulation of Apoptosis Apoptosis-Necrosis Cell Death Continuum Necroptosis Autophagy Important Mediators of Neurodegeneration Oxidative Stress Excitotoxic Amino Acids Mitochondrial Dysfunction, Energy Failure, and Ion Dysregulation Neuroinflammation Neurotrophin Support and Altered Cell Signaling Misfolded and Aggregated Proteins Gene Mutations, Noncoding RNAs, and Exosomes Pharmacological Intervention Inhibitors of Oxidative Stress Modulators of Glutamate Transmission Targeting Mitochondrial Dysfunction Neuroinflammation Inhibitors of Apoptosis, Necroptosis, and Growth Factor-Like Molecules Autophagy Inducers Other Investigational Approaches References Neurokinin A Receptor Neurokinin B Receptor Neurokinin/Tachykinin Receptors Synonyms Definition Basic Mechanisms Drugs References Neurokinin-1 Receptor Neurokinin-2 Receptor Neurokinin-3 Receptor Neuronal Cell Death Neuronal Cell Deterioration Neuropathology Neuropeptide Y Synonyms Definition Basic Characteristics Drugs References Neuroprotection Neuroprotection-Neurorescue Neurosteroids Definition Basic Characteristics Biosynthesis Regulation of Neuroplasticity Through Genomic Pathways Regulation of Neuroplasticity Through Non-genomic Pathways Behavioral Consequences Anxiolytic and Sedative Properties Effects on Memory Potential Use in Therapeutic Central Nervous System Injuries Epilepsy Stress-Related Disorders Conclusion Cross-References References Neurotransmission Neurotrophic Factors Synonyms Definition Mechanism of Action NT Family GFL Family Neurokine Family FGF Family TGF Family MANF and CDNF Family Clinical Use References Neurotrophins NFAT NFAT Family of Transcription Factors Synonyms Definition Basic Characteristics Structure of NFAT Proteins Regulation of NFAT Activation Transcriptional Activity Functions Drugs References NFAT5 NFATc1 NFATc2 NFATc3 NFATc4 NF-κB, Molecular Target Synonyms Definition Basic Characteristics NF-κB Structure NF-κB Activation Cellular Functions NF-κB and Immunity NF-κB, Inflammation and Inflammatory Diseases NF-κB, Cell Survival, Cell Proliferation, and Cancer Drugs Glossary References NGS Niacin Nicotinic Acetylcholine Receptor Nicotinic Receptors Synonyms Definition Basic Characteristics Drugs Therapeutic or Agrochemical Applications References Nitric Oxide Synonyms Definition Basic Mechanisms Enzymatic NO Synthesis Nonenzymatic NO production NO Donors NO Inactivation NO Receptor Physiological Effects of NO Endothelial NO Neuronal NO Inflammatory NO Pathophysiological Effects of NO Pharmacological Relevance References Nitrogen Monoxide Nitrogen(II) Oxide NMR NMR Spectroscopy Nonhomologous End Joining Nonreceptor Tyrosine Kinases Non-selective Cation Channels Synonyms Definition Basic Characteristics Drugs Cross-References References Non-specific Cation Channels Nonspecific ChE Nonviral Peptidases Synonyms Definition Basic Characteristics Active Site Residues Classification and Nomenclature Compound and Complex Peptidases Precursors and Zymogens Specificity and Substrate-Binding Drugs References NPY NSCCs Nuclear Magnetic Resonance Synonyms Definition Description Applications Synthetic Chemistry Quality Control Compound Identity Evaluation Protein Analysis Investigation of Biomolecular Structure and Dynamics by NMR Orthogonal Interaction Assays NMR-Based Screening Pharmaceutical Relevance References Nuclear Receptor Regulation of Hepatic Cytochrome P450 Enzymes Glossary Terms Definition Basic Mechanisms CYP1 Induction Via AhR Role of CAR in CYP2B Induction and Other Phenobarbital Responses CYP3A Induction by PXR: Role in Metabolism of Xenochemicals and Endogenous Lipophilic Substrates PPARα: Xenochemical Induction of CYP4A Enzymes and Role in Rodent Hepatocarcinogenesis Pharmacological Relevance Importance of Nuclear Receptors for Drug Metabolism and Drug Development Acknowledgments References O Omega-3 Fatty Acids 1,25(OH)2D3 14-3-3 Proteins Synonyms Definition Basic Mechanisms Recognizing Covalent Modifications 14-3-3 Sequence Conservation, Structure, and Function Modes of Action Binding Specificity Among 14-3-3 Isoforms 14-3-3 Interactome Pharmacological Intervention References Opioid Systems Definition Basic Characteristics Receptor Subtypes and Opioid Ligands Physiology Receptor Regulation Drugs Therapeutic Applications and Abuse References Oral Contraceptives Organ Dysfunction Ovarian Cancer G Protein-Coupled Receptor 1 (OGR1, GPR68) Oxygenated Derivative of Cholesterol Oxygenated Sterols Oxysterols Synonyms Definition and Introduction Nomenclature General Principles of Oxysterols Generators Modifiers Effectors Oxysterols, Disease, and Concluding Remarks References Oxytocin Synonyms Definition Basic Characteristics Oxytocin Receptor Activation Oxytocin Effects Parturition Lactation Copulation Hypothalamo-Pituitary-Gonadal Axis Natriuresis Behavioral Effects of Oxytocin Drugs Agonists Antagonists References P P1 Receptors P450 Monooxygenase System Synonyms Definition Basic Characteristics Cytochrome P450 Electron Transport Systems Cytochrome P450 Structure Cytochrome P450 Gene Superfamily Human Drug Metabolizing Cytochromes P450 Genetic Variation in Drug-Metabolizing P450s Gene Regulatory Mechanisms in Drug-Metabolizing P450s Direct Inhibition of P450 Drugs Human Drug-Metabolizing CYPs CYPs in Physiological Pathways References Pain Medication Parkinson´s Disease Pathogenesis PCSK9 Inhibition Peptides and Peptidomimetics as Foundations for Drug Discovery Synonyms Definition Peptides and Peptidomimetics The Role of Peptides and Peptidomimetics in Drug Discovery Somatostatin Basic Mechanisms Pharmacological Intervention Substance P Basic Mechanisms Pharmacological Intervention Polymyxins Basic Mechanisms Pharmacological Intervention References Peptidomimetics Pharmacokinetic and/or Pharmacodynamic Consequence of Multiple Drug Therapy Pharmacokinetic and/or Pharmacodynamic Interactions Pharmacology Phosphatidylinositide Kinases Phosphatidylinositol Kinases Phosphoinositol Kinases Phospholipid Kinases Synonyms Definition Basic Characteristics Classification of PI3Ks Protein Kinase Activity of PI3K Nonenzymatic Roles of PI3K Downstream Effectors of PI3Ks Drugs References Phosphoprotein Phosphatase Phthisis Physiology and Treatment of Hyperuricemia and Gout Synonyms Definition Basic Mechanisms Uric Acid Uric Acid Generation Urate Crystal Formation Uric Acid Clearance URAT1 Is the Predominant Urate Reabsorption Transporter Pharmacological Intervention Xanthine Oxidase Inhibitors (XOi) Uricosurics Urate Hydrolysis by Uricases Conclusions Cross-References References Physiology of Blood Pressure PIAS Proteins Definition Domain Structure and Function Characteristics of PIAS Proteins Drugs References Pitocin (Trade Name) PKC Placebo Effect Synonyms Definition Basic Mechanisms Methodological Considerations Psychological Mechanisms Neurobiology of Placebo Analgesia Parkinson´s Disease Immune and Endocrine Responses Depression Nocebo Effect Pharmacological Relevance Implications for Clinical Trials Hidden Administration of Drugs Prefrontal Control and Placebo Response References Placebo Response Plasma ChE Platelet Aggregation Inhibitors Platelet Inhibitors Plexins Definition Basic Mechanisms Pharmacological Intervention References Polymyxins Polypeptide Chain-Binding Proteins Posttranslational Protein Modification Pro-drug Prodrugs Synonyms Definition Basic Mechanisms Pharmacological Relevance Improving Solubility Improving Permeability Better Targeting References Propionylcholinesterase Proprotein Convertases Synonyms Definition Basic Characteristics PCs and Cardiovascular Diseases PCs and Cancer PCs and Viral/Bacterial Infections Drugs Inhibitors of Kexin-Like PCs Small Molecule Inhibitors Peptides PCSK9 Inhibitors Evolocumab and Alirocumab Translator Inhibitors Small Interference RNA References Proprotein-Convertases Subtilysin/Hexin Type 1-9 (PCSK 1-9) Pro-resolving Mediators Synonyms Definition Basic Characteristics Specialized Pro-resolving Lipid Mediators Protein and Peptide Pro-resolving Mediators Pro-resolving Receptor Signaling Gaseous Pro-resolving Signaling Pathophysiology and Therapeutic Potential Pathophysiology and Therapeutic Potential References Prostaglandin G/H Synthases Prostaglandin-Endoperoxide H Synthases (PGHSs) Prostanoids Definition Basic Characterization Biosynthesis and Degradation Formation of Prostanoids Degradation of Prostanoids Effects of Prostanoids PGE2 TXA2 and PGI2 PGD2 PGF2α Drugs References Protease-Activated Receptors (PARs) Synonyms Definition Basic Characteristics The Tethered Ligand Activation Mechanism Protease Activated Receptor Subtypes PAR1 PAR2 PAR3 PAR4 Drugs Blocking Antibodies Allosteric Modulators Small Molecule Antagonists PAR1 PAR2 PAR4 Single Nucleotide Polymorphisms (SNPs) Future Directions References Proteases Proteasome Inhibitors Synonyms Definition Mechanism of Action Proteasome Composition and Diversity Downstream Pathways that Contribute to Cell Death Classes of Drugs Boronates Epoxyketones Bicyclic β-Lactone γ-Lactams Clinical Use (Including Side Effects) References Protein Degradation Protein Kinase A Anchoring Proteins Protein Kinase C Synonyms Definition Basic Characteristics The PKC Family Regulation Function in Health and Disease Drugs Activators Inhibitors Cross-References References Protein Phosphatases Synonyms Definition Basic Mechanisms or Characteristics Widespread Protein Phosphorylation Protein Phosphatases and Kinases PPP Family of Protein Phosphatases PP1 PP2A/4/6 PP3 (PP2B/Calcineurin) PP5 PPM Family of Protein Phosphatases PTP Family of Protein Phosphatases Aspartate-Based Family of Protein Phosphatases Pharmacological Intervention References Protein S-Nitrosylation Synonyms Definition Basic Characteristics Generation of NO in Mammalian Cells Protein S-Nitrosylation Specificity of Protein S-Nitrosylation Examples of Neuroprotective Signaling Pathways Triggered by S-Nitrosylation in the Brain: S-Nitrosylation of NMDARs Examples of Neurodegenerative Signaling Pathways Triggered by Aberrant S-Nitrosylation in the Brain: S-Nitrosylation of Drp1 a... Drugs Affecting Protein S-Nitrosylation NitroSynapsin Deprenyl and CGP3466B (TCH346 or Omigapil) Disclosure of Conflicts of Interest References Protein Tyrosine Kinases Proteinases Proteolytic Enzymes Protocidal Drugs Proton-Sensing GPCRs Synonyms Definition Basic Characteristics Structure-Function Potential Physiological Roles of pH-Sensing Receptors Drugs Conclusions References Pseudocholinesterase Psychedelic Drugs Synonyms Definition Background Mechanism of Action Anti-inflammatory Properties Clinical Uses Effects of Psychedelics on Functional Brain Dynamics References Psycho Analeptics Psycho Energizers Psychomotor Stimulant Drugs Psychostimulants Synonyms Definition Mechanism of Action General Remarks Methylphenidate, Amphetamine, and Cocaine Modafinil Nicotine Clinical Use Cross-References References Psychotomimetic PT-141 Pulmonary Arterial Hypertension Synonyms Definition Basic Mechanisms Vasoreactivity Pulmonary Vascular Remodeling Genetic Mutations Signaling Abnormalities Metabolism and Hypoxia Inflammation Summary References Pulmonary Emphysema Pulmonary Vascular Disease Pulmonary Vascular Remodeling Purinergic System Definition Basic Characteristics Purinoceptor Subtypes Physiology Short-Term Neuronal Signaling Short-Term Nonneuronal Signaling Long-Term (Trophic) Signaling Pathophysiology and Therapeutic Potential References Q Quantification of Drug Effect R RAAS RAD24 RAD25 Regulation of Ingestive Behavior Regulation of Smooth Muscle Contractility Rel Proteins Relaxin Relaxin Family Peptides and Their Receptors Synonyms Definition Basic Characteristics Drugs References Relaxin-3 Renin-Angiotensin System (RAS) Renin-Angiotensin-Aldosterone System Synonyms Definition Basic Characteristics General Adrenal Gland Kidney Heart and Vessels Brain Alternative RAS Drugs ACE Inhibitors AT1 Antagonists Renin Inhibitors Vasopeptidase Inhibitors Aldosterone Antagonists Cross-References References Reslizumab Retinoic Acid Retinoids Synonyms Definition Basic Mechanisms Transport, Biosynthesis, Metabolism Nuclear and Nongenomic Signaling Pathways of RARs Various Classes of RAR Modulators Structural Basis of Ligand Activity RAR-Subtype Selective Retinoids Pharmacological Relevance Retinoids in Medical Use Retinoids as Pharmacological Tools References Rheumatoid Arthritis Synonyms Definition Basic Mechanisms Characteristics Cellular Pathology Genetic Factors Cytokines Role of Cytokines in the Pathogenesis of RA Pharmacological Intervention Cross-References References RNA-Sequencing RXFP1 RXFP2 RXFP3 RXFP4 Ryanodine Receptor Synonyms Definition Basic Characteristics Occurrence and Role Structure Ca2+ Release Mechanisms CICR and Its Endogenous Modulators E-C Coupling in Skeletal Muscle E-C Coupling in Heart Diseases Drugs Ryanodine Caffeine 4-Chloro-m-cresol (4-CmC) Inhalational Anesthetics FK506 and Rapamycin Dantrolene Procaine and Tetracaine Ruthenium Red References S S100 Proteins Synonyms Definition Basic Characteristics Clinical Importance of S100 Proteins in Human Diseases Cardiology Oncology Inflammation, Autoimmune Diseases and Allergies Brain Injury and Neuropathologies Drugs Outlook References SAR-by-NMR Synonyms Definition Basic Characteristics References Scaffold Second-Generation Antipsychotics Sedation sEH Seminiferous Epithelial Barrier Senescence Synonyms Definition Basic Mechanisms Inducers Hallmarks, Molecular Pathways, Markers Physiological and Pathological Implications Pharmacological (Therapeutic) Intervention Senolytics Senomorphics or Senostatics (SASP Inhibitors) Modifiers/Enhancers of the Immune System Nanoparticles Acknowledgments References Sepsis Synonyms Definition Basic Mechanisms Immune Responses The Role of Parenchymal Tissues Molecular Mechanisms Mediating (Mal-)adaptive Responses to Infection Pharmacological Intervention Current Standard of Care Novel Treatment Approaches - Restoring Immune and Organ Function Cross-References References Septic Shock Serine/Threonine Protein Kinase Phosphorelay Modules Serotonergic Hallucinogen Serotonin Serotoninergic System Synonyms Definition Basic Characteristics Physiology Multiple 5-HT Receptor Subtypes Pathophysiology/Clinical Applications Cross-References References Sertoli Cell Barrier Severe Eosinophilic Asthma Sex Steroid Receptors: Androgen Receptor, Estrogen Receptors, Progesterone Receptor Definition Basic Characteristics Androgen Receptor Estrogen Receptor ERα ERβ Progesterone Receptor Drugs References Silent Information Regulator 2 (Sir2) Proteins Sirtuins Synonyms Definition Basic Characteristics of Sirtuins Physiopathological Characteristics of Sirtuins Sirtuin Modulators Sirtuin Inhibitors (SIRTi) Small Molecules Peptides and Pseudopeptides SIRT Activators Cross-References References Skeletal Metabolism Skeletal Turnover Small G Proteins Small GTPases Synonyms Definition Basic Characteristics Regulation General Structural Properties Posttranslational Modification Families Ras GTPases Rho GTPases Rab GTPases Arf/Sar1 GTPases Ran GTPases Cascades and Cross-Talk Drugs Cross-References References Small Molecules Small-Molecule Screens Synonyms Definition Description Small Molecule Small-Molecule Screens Pharmacological Relevance Common Screening Technologies References Smooth Muscle Tone Regulation Synonyms Definition Basic Mechanisms Calcium-Dependent Contraction Calcium-Independent Contraction Relaxation of Smooth Muscle Pharmacological Intervention References S-Nitrosation Sodium- and Potassium-Activated Adenosine 5′-Triphosphatase (EC 7.2.2.13) Sodium Calcium Exchanger Sodium Pump Sodium/Proton Antiporter Sodium/Proton Exchanger Soluble Epoxide Hydrolase Synonyms Definition Basic Characteristics Metabolism of PUFAs Hydrolysis of EpFAs Mechanism of sEH Inhibition Biological Action of EETs and EpFAs Drugs Representative sEH Inhibitors Acknowledgments References Solute Carrier 9 Family Somatostatin Definition Basic Characteristics Somatostatin and Somatostatin-Related Peptides Tissue Distribution Physiology Somatostatin Receptor Subtypes Agonist-Dependent Receptor Regulation Drugs SRIF Analogs in Clinical Practice SRIF-Based Radiopharmaceuticals Cross-References References Specialized Pro-resolving Lipid Mediators Sphingosine-1-Phosphate Definition Basic Characteristics Metabolism and Occurrence S1P Receptors Biological Actions Drugs References SPMs Statins Steroids Stimulant Drugs Stimulants Stress Proteins Stroke Definition Basic Mechanisms Ischemic Penumbra Pathomechanisms of Ischemic Brain Damage Pharmacological Intervention/Pharmacotherapy Future Directions References Structural Bioinformatics Strychnine-Sensitive Glycine Receptor sUA Substance P Substance P Receptor Substantia Nigra Synapse Synaptic Transmission Synonyms Definition Basic Mechanisms Transmitter Synthesis and Vesicular Storage Glutamate and GABA Acetylcholine Monoamines Neuropeptides Transmitter Release Docking and Priming Exocytosis Stochastic Release Postsynaptic Receptor Activation Ligand-Gated Ion Channels (LGIC) LGIC/Glutamate Receptors LGIC/GABAA- and Glycine Receptors G Protein-Coupled Receptors (GPCRs) GPCR/Gαi/o Coupling GPCR/Gαq/11 and Gαs Coupling Termination of Synaptic Transmission Extracellular Degradation of Transmitters Elimination of Transmitters by Transporters Modulation of Synaptic Transmission Presynaptic Receptors Retrograde Signaling Clinical Pharmacology: Drugs Interfering with Synaptic Transmission Transmitter Production and Vesicular Storage Transmitter Release Postsynaptic Receptor Activation Transmitter Inactivation Cross-References References Synthetic Lethality Syntocinon Systemic Inflammation T T Cell Death-Associated Gene 8 (TDAG8, GPR65) Tachykinin 1 Receptor Tachykinin 2 Receptor Tachykinin 3 Receptor TGF-β Pathway Synonyms Definition Basic Characteristics TGF-β Pathway Canonical TGF-β-SMAD Signaling Non-SMAD Signaling Physiological Roles of TGF-β Signaling TGF-β Mediates Regulation of Gene Expression TGF-β Controls Cell Proliferation and Differentiation TGF-β Induces Epithelial-to-Mesenchymal Transition TGF-β Regulates Wound Healing TGF-β Mediates Regulation of the Immune System Pathologies Resulting from Deregulated TGF-β Signaling Fibrosis Cancer Drugs Pharmacological Agents Targeting TGF-β Signaling Acknowledgments References TGF-β Signaling Pathway TGF-β/SMAD Pathway Therapy Thionamides Thrombin Receptor Thymoleptics Tinzaparin T-Kinin (Ile-Ser-Bradykinin) Trace Amine-Associated Receptors Definition Basic Characteristics Invertebrates Synthesis, Storage, Release, and Degradation Involvement in Disorders Mechanisms of Action Receptors TAAR1 Other Receptors TAAR Receptors in Olfaction Drugs Conclusion References Transcription Factors Transcriptional Regulation Synonyms Definition Basic Mechanisms Background Transcription Initiation Promoters Enhancers Epigenetic Regulation of Transcription The Histone Code Pharmacological Relevance References Transcriptome Analysis Transforming Growth Factor-Beta Pathway Transient Receptor Potential Channels TRP Channels Synonyms Definition Basic Characteristics Ion Channel Properties Modes of Activation Pharmacological Relevance Biological Relevance and Emerging Roles for Mammalian TRP Channels References True ChE Tuberculosis Synonyms Definition Basic Mechanisms The Disease The Agent The Control The Exacerbation Pharmacological Intervention Classical Treatment Multi-drug- and Extensively Drug-Resistant Tuberculosis Host-Directed Therapy References 24h-Rhythms Tyrosine Kinases Synonyms Definition Basic Characteristics c-Src c-Abl Fak Jak Tec Syk Drugs References Tyrosine-Protein Kinase JAK Tyrosylprotein Kinase U Ubiquitin/Proteasome Synonyms Definition Basic Mechanisms Ubiquitin Conjugation Ubiquitin Modification as a Signal for Proteasomal Degradation Non-proteolytic Functions of Ubiquitin Conjugation Ubiquitin-Like Proteins Disease Associated with Perturbations of the Ubiquitin System Pharmacological Intervention Pharmacologic Targeting of Components of Ubiquitin and Ubiquitin-Like Modification Systems Pharmacologic Exploitation of the Ubiquitin Proteasome System for Targeted Degradation of Proteins References Unfolded Protein Response Synonyms Definition Basic Characteristics of UPR Pathway Characteristics of IRE1α Signaling Characteristics of PERK Signaling Characteristics of ATF6 Signaling Therapeutic Approach to Modulate UPR IRE1α RNase Inhibitors Allosteric IRE1α Kinase Modulators Inhibitors of PERK Signaling elf2α Phosphatase Blockers ATF4 Inhibitors or elf2B Activator ATF6 Modulators Future Prospective References URAT1 V Vascular Natriuretic Peptide Vasopressin Synonyms Definition Basic Characteristics Vasopressin Receptor Activation Vasopressin Effects Antidiuretic Action Osmoreception Cardiovascular Function Behavioral Effects Drugs Agonists Antagonists References Ventral Tegmental Area (VTA) Viral Peptidases Viral Proteases Synonyms Definition Basic Characteristics Drugs Aspartyl Proteases HIV-1 Protease Serine Proteases Hepatitis C Protease Flavivirus Protease Alphavirus Protease Herpesvirus Protease Cysteine Proteases Coronavirus Protease References Viral Proteinases Viral Vectors Vitamin A Metabolites Vitamin D Synonyms Definition Mechanism of Action In Vivo Production of Vitamin D Metabolic Enzymes and Their Regulation Other Metabolites Lithocholic Acid 3-epi-25(OH)D3 and 3-epi-1,25(OH)2D3 25,26(OH)2D3 and 1,25,26(OH)3D3 24,25(OH)2D3 Clinical Uses References Vitamin K Synonyms Definition Mechanisms of Action General Aspects Influence on Cell Functions via Gas6 Coagulation Bone Mineralization Clinical Use (Including Side Effects) Vitamin K Deficiency Osteoporosis Atherosclerosis Safety and Toxicity Cross-References References Voltage-Dependent Ca2+ Channels Synonyms Definition Basic Characteristics Mutation and Deletion Drugs References Voltage-Gated K+ Channels Synonyms Definition Basic Characteristics Functional Characteristics Structural Characteristics of Kv-Channels Auxiliary Subunits Drugs Mutations in Human Kv-Genes Associated with Hereditary Channelopathies Outlook Cross-References References VYLEESI W Wall Peptidoglycan Inhibitors Water Channels Weight-Loss Therapies Weight-Management Pharmacotherapy White Plague Wnt Signaling Definition Basic Mechanism Insight into Posttranslational Modification of Wnts Glycosylation of Wnts Fatty Acylation of Wnts Insight into Secretion of Wnt Proteins Insight into Transportation of Secreted Extracellular Wnts Insight into Wnt Signaling Canonical Wnt Signaling Noncanonical Wnt Pathway Extracellular Wnt Regulation Wnt Antagonists Wnt-YAP/TAZ Interplay Modulation by R-spondin (RSPO) Decarboxylation of Acylated Wnts by Notum Drugs References X XNPEP2 Z Zinc-Binding
