Drugs, their targets and the nature and number of drug targets

5-Fluorouracil: mechanisms of action and clinical strategies

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Cisplatin: mode of cytotoxic action and molecular basis of resistance

2003 • 3,150 citations

The druggable genome

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Prostanoid Receptors: Structures, Properties, and Functions

1999 • 2,395 citations

A Transmembrane Intracellular Estrogen Receptor Mediates Rapid Cell Signaling

2005 • 2,191 citations

Mechanism of Action of Fibrates on Lipid and Lipoprotein Metabolism

1998 • 1,690 citations

Functional insights from the structure of the 30S ribosomal subunit and its interactions with antibiotics

2000 • 1,554 citations

Mycophenolate mofetil and its mechanisms of action

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Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors.

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The retinoids—Biology, chemistry and medicine

1996 • 1,192 citations

The proteasome: a suitable antineoplastic target

2004 • 1,189 citations

Value of low dose combination treatment with blood pressure lowering drugs: analysis of 354 randomised trials

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Designed Multiple Ligands. An Emerging Drug Discovery Paradigm

2005 • 1,111 citations

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

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Echinocandin antifungal drugs

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3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain

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Artemisinins target the SERCA of Plasmodium falciparum

2003 • 1,017 citations

Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria

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Biological basis for the cardiovascular consequences of COX-2 inhibition: therapeutic challenges and opportunities

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Molecular recognition of DNA by small molecules

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Statins: mechanism of action and effects

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Structure and function of dopamine receptors

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Approaches to the Description and Prediction of the Binding Affinity of Small-Molecule Ligands to Macromolecular Receptors

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CD28-dependent Rac1 activation is the molecular target of azathioprine in primary human CD4+ T lymphocytes

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Molecular Physiology and Pathophysiology of Electroneutral Cation-Chloride Cotransporters

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Serotonin receptors : their key role in drugs to treat schizophrenia

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Multicomponent therapeutics for networked systems

2005 • 749 citations

The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)

2005 • 743 citations

Sirolimus: its discovery, biological properties, and mechanism of action

2003 • 717 citations

Diabetes mellitus : a fundamental and clinical text

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Chemistry, Biology, and Medicine of the Glycopeptide Antibiotics

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Advances in H₁-Antihistamines

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Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.

1994 • 650 citations

The Structure−Activity Relationship between Peroxisome Proliferator-Activated Receptor γ Agonism and the Antihyperglycemic Activity of Thiazolidinediones

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Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.

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Quinoline Antimalarials Mechanisms of Action and Resistance and Prospects for New Agents

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Heparin: Mechanism of Action, Pharmacokinetics, Dosing Considerations, Monitoring, Efficacy, and Safety

1992 • 548 citations

The Molecular Basis of Thyroid Hormone Action

1994 • 541 citations

Platelet GPIIb-IIIa blockers

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Modes of action of anthelmintic drugs

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Bleomycin: New Perspectives on the Mechanism of Action

1999 • 522 citations

Caffeine as a psychomotor stimulant: mechanism of action

2004 • 509 citations

Chemistry and Structural Biology of Androgen Receptor

2005 • 496 citations

Angiotensin II Type 1 Receptor Blockers

2001 • 477 citations

Real-time measurement of dopamine fluctuations after cocaine in the brain of behaving rats

2005 • 473 citations

L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase

1995 • 472 citations

Organophosphate Pesticides: Biochemistry and Clinical Toxicology

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Pharmacology of cardiac potassium channels

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Histone Deacetylase Is a Target of Valproic Acid-Mediated Cellular Differentiation

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Conversion of Acetaminophen to the Bioactive N-Acylphenolamine AM404 via Fatty Acid Amide Hydrolase-dependent Arachidonic Acid Conjugation in the Nervous System

2005 • 430 citations

History of the development of azole derivatives

2004 • 429 citations

Sorafenib (BAY 43‐9006, Nexavar®), a Dual‐Action Inhibitor That Targets RAF/MEK/ERK Pathway in Tumor Cells and Tyrosine Kinases VEGFR/PDGFR in Tumor Vasculature

2006 • 422 citations

The Neuropharmacological Basis for the Use of Memantine in the Treatment of Alzheimer's Disease

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Molecular Physiology of Norepinephrine and Serotonin Transporters

1994 • 404 citations

Mechanism of action of hydroxyurea.

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Knockouts model the 100 best-selling drugs—will they model the next 100?

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A proton-pump inhibitor expedition: the case histories of omeprazole and esomeprazole

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Biochemical mechanisms of drug action: what does it take for success?

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Mechanisms of Action of Antiepileptic Drugs

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Heparin: Mechanism of Action, Pharmacokinetics, Dosing Considerations, Monitoring, Efficacy, and Safety

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Pharmacodynamics of the Type II Calcimimetic Compound Cinacalcet HCl

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Pharmacokinetics and Pharmacodynamics of the Nitroimidazole Antimicrobials

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Progress Towards the Discovery of Xanthine Oxidase Inhibitors

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The camptothecins

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ACTIONS OF ADENOSINE AT ITS RECEPTORS IN THE CNS: Insights from Knockouts and Drugs

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Mode of action of orlistat.

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Playing dirty

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Relibase: Design and Development of a Database for Comprehensive Analysis of Protein–Ligand Interactions

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Structure and function of the Mur enzymes: development of novel inhibitors

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Pegaspargase: a review of clinical studies

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Fluoroquinolones: Action and Resistance

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Functional role of M₂ and M₃ muscarinic receptors in the urinary bladder of rats in vitro and in vivo

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Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology

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What Are the Right Targets for Psychopharmacology?

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Crystal structure of the anti-bacterial sulfonamide drug target dihydropteroate synthase

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Refined crystal structures of Escherichia coli and chicken liver dihydrofolate reductase containing bound trimethoprim.

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Mechanisms of action of carbamazepine and its derivatives, oxcarbazepine, BIA 2-093, and BIA 2-024.

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P2Y12, a New Platelet ADP Receptor, Target of Clopidogrel

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Botulinum Toxin: Mechanisms of Action

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Structural basis of drug binding to L Ca2+ channels

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The anandamide transport inhibitor AM404 activates vanilloid receptors

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Trapping of a Methanesulfonanilide by Closure of the Herg Potassium Channel Activation Gate

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1,4-Dihydropyridines as calcium channel ligands and privileged structures.

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Mechanistic Basis of Enzyme-Targeted Drugs

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DNA sequence selectivity of guanine–N7 alkylation by nitrogen mustards

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Mode of antiviral action of penciclovir in MRC-5 cells infected with herpes simplex virus type 1 (HSV-1), HSV-2, and varicella-zoster virus

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An essential role for mitochondrial aldehyde dehydrogenase in nitroglycerin bioactivation

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Amiodarone: ionic and cellular mechanisms of action of the most promising class III agent

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Research and Development of Donepezil Hydrochloride, a New Type of Acetylcholinesterase Inhibitor

2002 • 216 citations

Block of Cloned Human T-Type Calcium Channels by Succinimide Antiepileptic Drugs

2001 • 211 citations

Mechanism of Action of Anti-Her2 Monoclonal Antibodies: Scientific Update on Trastuzumab and 2c4

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CD33-directed therapy with gemtuzumab ozogamicin in acute myeloid leukemia: progress in understanding cytotoxicity and potential mechanisms of drug resistance

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.alpha.- and .beta.-Adrenoceptors: From the Gene to the Clinic. Part 1. Molecular Biology and Adrenoceptor Subclassification

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Unfolding the Action of Progesterone Receptors

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Update on colchicine and its mechanism of action

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.alpha.- and .beta.-Adrenoceptors: From the Gene to the Clinic. 2. Structure-Activity Relationships and Therapeutic Applications

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The β-lactamase cycle: a tale of selective pressure and bacterial ingenuity

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New windows on the mechanism of action of KATP channel openers

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The bacA Gene of Escherichia coli Encodes an Undecaprenyl Pyrophosphate Phosphatase Activity

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Potential of Substance P Antagonists as Antiemetics

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Inhibitors of fatty acid synthesis as antimicrobial chemotherapeutics

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What is the evidence that oxcarbazepine and carbamazepine are distinctly different antiepileptic drugs?

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Target sites of anthelmintics

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Drugs targeting the ribosome

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Pharmacology of cannabinoids.

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Therapeutic opportunities from muscarinic receptor research

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Drug Development: The role of innovation in drug development

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Lithium and valproic acid: parallels and contrasts in diverse signaling contexts

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The blood coagulation system as a molecular machine

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Etoposide: Discovery and Medicinal Chemistry

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Alterations at the peptidyl transferase centre of the ribosome induced by the synergistic action of the streptogramins dalfopristin and quinupristin.

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The enzymology of prostaglandin endoperoxide H synthases-1 and -2

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Diamine Oxidase: An Overview of Historical, Biochemical and Functional Aspects

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Novel Aspects of Natural and Modified Vinca Alkaloids

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The pharmacology of ergotamine and dihydroergotamine.

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Are Ca2+ channels targets of praziquantel action?

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Aromatase inhibitors: mechanism of action and role in the treatment of breast cancer

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Neuromuscular block

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Targeting DHFR in parasitic protozoa

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Characteristics of catechol O-methyltransferase (COMT) and properties of selective COMT inhibitors

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Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP−Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor

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Selective oestrogen receptor modulation

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Ethanol and amino acids in the central nervous system: assessment of the pharmacological actions of acamprosate

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Vasopressin and terlipressin: pharmacology and its clinical relevance

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Nitrates and no release: contemporary aspects in biological and medicinal chemistry

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Cross-linking in the Living Cell Locates the Site of Action of Oxazolidinone Antibiotics

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Galantamine is an allosterically potentiating ligand of the human α4/β2 nAChR

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The structures of prostaglandin endoperoxide H synthases-1 and -2

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Lignans Isolated from Valerian: Identification and Characterization of a New Olivil Derivative with Partial Agonistic Activity at A₁ Adenosine Receptors

2002 • 143 citations

Molecular Biology of Opioid Analgesia

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Cholinergic Stimulation of Salivary Secretion Studied with M₁ and M₃ Muscarinic Receptor Single- and Double-Knockout Mice

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Sunitinib maleate

2006 • 137 citations

Molecular action of androgens

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Insulin Secretagogues, Sulfonylurea Receptors and KATP Channels

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Androgen Receptor: Structural Domains and Functional Dynamics after Ligand‐Receptor Interaction

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Mechanism of action of leflunomide in rheumatoid arthritis.

1998 • 129 citations

Basic and clinical pharmacology of new motility promoting agents

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GABAA receptor subtypes: any clues to the mechanism of benzodiazepine dependence?

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Current Understanding of the Function of the Nuclear Vitamin D Receptor in Response to Its Natural and Synthetic Ligands

2003 • 125 citations

Towards a mechanism-based analysis of pharmacodynamic drug?drug interactions in vivo

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Where do triptans act in the treatment of migraine?

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Abciximab (c7E3 Fab)

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Is the calcium receptor a molecular target for the actions of strontium on bone?

2003 • 123 citations

New Approaches to Influenza Chemotherapy

1998 • 122 citations

Biochemistry and Molecular Biology of the Vesicular Monoamine Transporter from Chromaffin Granules

1994 • 119 citations

The mechanisms of action of disease-modifying antirheumatic drugs: A review with emphasis on macrophage signal transduction and the induction of proinflammatory cytokines

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Calcineurin inhibitors and sirolimus: mechanisms of action and applications in dermatology

2002 • 119 citations

Structure of the Ferrous Form of (4-Hydroxyphenyl)pyruvate Dioxygenase from Streptomyces avermitilis in Complex with the Therapeutic Herbicide, NTBC^,

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Illuminating drug discovery with biological pathways

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Selective oestrogen receptor modulation

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Muromonab CD‐3: A Review of Its Pharmacology, Pharmacokinetics, and Clinical Use in Transplantation

1991 • 111 citations

Propranolol, a phosphatidate phosphohydrolase inhibitor, also inhibits protein kinase C.

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The pharmacology and toxicology of disulfiram and its metabolites

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Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters

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P2Y₁₂, A New Platelet ADP Receptor, Target of Clopidogrel

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Molecular Pharmacology of Topiramate: Managing Seizures and Preventing Migraine

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The mechanism of action of terbinafine

1989 • 106 citations

Carbamazepine is an inhibitor of histone deacetylases

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After 130 years, the molecular mechanism of action of nitroglycerin is revealed

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Molecular Basis of Buspirone's Anxiolytic Action

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Membrane Targeted Anticancer Drugs: Potent Inducers of Apoptosis and Putative Radiosensitisers

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Heparins and Heparinoids: Occurrence, Structure and Mechanism of Antithrombotic and Hemorrhagic Activities

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A functional-phylogenetic system for the classification of transport proteins

1999 • 94 citations

Novel Mechanisms of Action of Three Antiepileptic Drugs, Vigabatrin, Tiagabine, and Topiramate

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Interactions between Cardiac Glycosides and Sodium/Potassium-ATPase: Three-Dimensional Structure−Activity Relationship Models for Ligand Binding to the E₂-P_i Form of the Enzyme versus Activity Inhibition

2004 • 93 citations

Activation of human plasminogen by equimolar levels of streptokinase.

1977 • 92 citations

Anakinra: an inhibitor of IL-1 for the treatment of rheumatoid arthritis

2004 • 91 citations

Behavioral and biochemical investigations of bupropion metabolites

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Structural Determinants for Branched-chain Aminotransferase Isozyme-specific Inhibition by the Anticonvulsant Drug Gabapentin

2005 • 88 citations

Pregabalin

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Molecular, biochemical, and cellular pharmacology of pemetrexed

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The antiandrogen cyproterone acetate: discovery, chemistry, basic pharmacology, clinical use and tool in basic research^*

2009 • 86 citations

Antiepileptic Drug Cellular Mechanisms of Action: Where Does Lamotrigine Fit In?

1997 • 86 citations

Molecular mechanisms of polyamine analogs in cancer cells

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Inhibitory Mechanism of Papaverine on Carbachol-Induced Contraction in Bovine Trachea

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Flumazenil: a benzodiazepine antagonist.

1993 • 81 citations

TiPS nomenclature supplement 2001

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Vitamin D Receptor as a Drug Discovery Target

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Adapalene biochemistry and the evolution of a new topical retinoid for treatment of acne

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Cetuximab

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Mouse models to study L-type calcium channel function

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A Side Reaction of Alanine Racemase: Transamination of Cycloserine^,

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Molecular, biochemical, and cellular pharmacology of pemetrexed

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Identification of Dantrolene Binding Sites in Porcine Skeletal Muscle Sarcoplasmic Reticulum

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Modulation of protein kinase C in antitumor treatment

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Bevacizumab

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Identification of an Amiloride Binding Domain within the α-Subunit of the Epithelial Na+ Channel

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Pharmacology of Drugs for Hyperuricemia

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The crystal structure of the complex between a disaccharide anthracycline and the DNA hexamer d(CGATCG) reveals two different binding sites involving two DNA duplexes

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Insights into the mechanisms of action of the MAO inhibitors phenelzine and tranylcypromine: a review.

1992 • 70 citations

Alemtuzumab

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Fondaparinux sodium: A selective inhibitor of factor Xa

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Lincosamides: Chemical Structure, Biosynthesis, Mechanism of Action, Resistance, and Applications

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Trends in Virtual Combinatorial Library Design

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Retinoid receptors in transcriptional regulation

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High-affinity ivermectin binding to recombinant subunits of the Haemonchus contortus glutamate-gated chloride channel

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Mineralocorticoid receptor binding, structure and function

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Alternatively spliced isoform of apical Na⁺-K⁺-Cl⁻cotransporter gene encodes a furosemide-sensitive Na⁺-Cl⁻cotransporter

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Exenatide

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Miglustat

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Ergosterol biosynthesis inhibition: a target for antifungal agents.

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Update on the mechanism of action of bimatoprost: a review and discussion of new evidence

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Daclizumab

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Adalimumab

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β-Lactams as Inhibitors of Serine Enzymes

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The role of aminosalicylates at the beginning of the new millennium in the treatment of chronic inflammatory bowel disease

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alpha-Glucosidases.

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How receptor mosaics decode transmitter signals. Possible relevance of cooperativity

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Molecular Biology and Pharmacology of PDE‐5—Inhibitor Therapy for Erectile Dysfunction

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Lercanidipine: a novel lipophilic dihydropyridine calcium antagonist with long duration of action and high vascular selectivity

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Discovery and mechanism of action of pegvisomant

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Identification and characterization of the catecholamine transporter in bovine chromaffin granules using [3H]reserpine.

1984 • 47 citations

Palivizumab

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Wirkmechanismen von Ketamin

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Antiretrovirals, Part II: Focus on Non-Protease Inhibitor Antiretrovirals (NRTIs, NNRTIs, and Fusion Inhibitors)

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Antiretrovirals, Part 1: Overview, History, and Focus on Protease Inhibitors

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Targeted drugs in metastatic colorectal cancer with special emphasis on guidelines for the use of bevacizumab and cetuximab: An Acta Oncologica expert report

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Mechanism of Action of Plasminogen Activators

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Killing and mutagenic actions of dacarbazine, a chemotherapeutic alkylating agent, on human and mouse cells: effects of Mgmt and Mlh1 mutations

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Probing conformational changes in neurotransmitter transporters: a structural context

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Granisetron: relating pharmacology to clinical efficacy

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Pharmacology of moclobemide.

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Molecular determinants of glucagon receptor signaling

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The role of leukotriene inhibitors in patients with paranasal sinus disease

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Potent block of Cl− channels by antiallergic drugs

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Structural Enzymology of Li+-sensitive/Mg2+-dependent Phosphatases

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Biochemical and Mechanistic Basis for the Activity of Nucleoside Analogue Inhibitors of HIV Reverse Transcriptase

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Basiliximab, mechanism of action and pharmacological properties.

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Mutschler Arzneimittelwirkungen

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Molecular basis of ligand binding and receptor activation in the oxytocin and vasopressin receptor family

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G Protein-Coupled Receptor Structural Motifs: Relevance to the Opioid Receptors

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The structural basis of ClC chloride channel function

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Cancer Chemoprevention Drug Targets

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The mechanisms underlying the unique pharmacodynamics of nateglinide

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Infliximab

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Yttrium-90-ibritumomab tiuxetan radioimmunotherapy: A new treatment approach for B-cell non-Hodgkin's lymphoma

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Cyclic GMP as the mediator of molsidomine-induced vasodilation

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Malaria Parasites Are Rapidly Killed by Dantrolene Derivatives Specific for the Plasmodial Surface Anion Channel

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Alteration of Lithium Pharmacology through Manipulation of Phosphoadenosine Phosphate Metabolism

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Mécanismes d’action des statines et des fibrates

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Flecainide

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The Thiazide-Sensitive Na-Cl Cotransporter and Human Disease

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Crystallization of the human glucocorticoid receptor ligand binding domain: a step towards selective glucocorticoids

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The soluble tumor necrosis factor receptor etanercept: A new strategy for the treatment of autoimmune rheumatic disease

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Library Design Practices for Success in Lead Generation With Small Molecule Libraries

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Mechanism of action of amiloride: a molecular prospective.

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Chiral Differentiation of DNA Adducts Formed by Enantiomeric Analogues of Antitumor Cisplatin Is Sequence-Dependent

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ACTH 1-24 inhibits proliferation of adrenocortical tumors in vivo

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Erlotinib hydrochloride

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G-protein-coupled receptors in drug discovery

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Comparative effects of K+ channel modulating agents on contractions of rat intestinal smooth muscle

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Aldesleukin in advanced renal cell carcinoma

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Clinical applications of colony-stimulating factors: A historical perspective

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Effect of oxiconazole and Ro 14-4767/002 on sterol pattern inCandida albicans

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Efalizumab

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Antiarrhythmic Drugs:

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Omalizumab: A Novel Therapy for Allergic Asthma

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Natalizumab

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Neuromuscular blockers in surgery and intensive care, Part 1

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The molecular physiology of erythropoietin and the erythropoietin receptor.

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Modulation of insulin signalling by insulin sensitizers

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Mapping of the second tetracycline binding site on the ribosomal small subunit of E.coli

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Histamine and its actions on isolated tissues of lower vertebrates.

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The challenge of regulating anticoagulant drugs: Focus on warfarin

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Biochemistry of Serine Protease Inhibitors and Their Mechanisms of Action: A Review

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Relationships between structure and vascular activity in a series of benzylisoquinolines

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Imipenem-Cilastatin Sodium, A Broad-Spectrum Carbapenem Antibiotic Combination

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Purification, kinetics and inhibition by antimonials of recombinant phosphofructokinase from Schistosoma mansoni

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Evaluation of enkephalinase inhibition in the living mouse, using [3H]acetorphan as a probe.

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Selective antagonists reveal different functions of M cholinoceptor subtypes in humans.

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Verapamil, a Ca2+ Entry Blocker, Targets the Pore-Forming Subunit of Cardiac Type KATP Channel (Kir6.2)

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³²P-Postlabeling Analysis of Binding of the Cyclophosphamide Metabolite, Acrolein, to DNA

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Pharmacology of bipyridine phosphodiesterase III inhibitors.

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TiPS Receptor Nomenclature Supplement. January 1992.

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Non-nucleoside reverse transcriptase inhibitors—an overview

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Effect of lamotrigine on the activities of monoamine oxidases A and B in vitro and on monoamine disposition in vivo

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Suramin Inhibits Proliferation and DNA Synthesis in Transitional Carcinoma Cell Lines

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The pharmacology of histamine H2-receptor antagonists.

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Rationales Design von Hemmern: Vom Teprotid zum Captopril

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The differentiation of propafenone from other class Ic agents, focusing on the effect on ventricular response rate attributable to its beta-blocking action

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A classification of drug substances according to their mechanism of action.

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Wirksamkeit und Toxizität der Taxane: Therapie solider Tumoren

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Pharmacodynamic properties of leukotriene receptor antagonists.

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Thermodynamic study of the interaction of methotrexate, its metabolites, and new antifolates with thymidylate synthase: Influence of FdUMP

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The interactions of phenytoin and its binding site in DI‐S6 segment of Na⁺ channel voltage‐gated peptide by NMR spectroscopy and molecular modeling study

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Crystallization and Preliminary X-Ray Crystallographic Analysis of UDP-N-Acetylglucosamine Enolpyruvyl Transferase from Haemophilus influenzae in Complex with UDP-N-Acetylglucosamine and Fosfomycin

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Potassium and magnesium retaining triamterene derivatives.

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Rational Design of ACE Inhibitors

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