Molecular Alliance-From Orthosteric and Allosteric Ligands to Dualsteric/Bitopic Agonists at G Protein Coupled Receptors

Structure of the δ-opioid receptor bound to naltrindole

(2012) Sébastien Granier et al.   NATURE

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

(2012) Kazuko Haga et al.   NATURE

Structure of the human κ-opioid receptor in complex with JDTic

(2012) Huixian Wu et al.   NATURE

Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic

(2012) Aaron A. Thompson et al.   NATURE

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

(2012) Aashish Manglik et al.   NATURE

Structure and dynamics of the M3 muscarinic acetylcholine receptor

(2012) Andrew C. Kruse et al.   NATURE

Structure-based drug screening for G-protein-coupled receptors

(2012) Brian K. Shoichet et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease

(2012) Michael Decker et al.   MedChemComm

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling

(2012) Andreas Bock et al.   Nature Communications

The Golden Age of GPCR Structural Biology: Any Impact on Drug Design?

(2011) Peter Kolb et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

(2011) Celine Valant et al.   Annual Review of Pharmacology and Toxicology

“Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology

(2011) Michael R. Wood et al.   BIOCHEMISTRY

Pharmacological modulation of chemokine receptor function

(2011) DJ Scholten et al.   BRITISH JOURNAL OF PHARMACOLOGY

Biased signalling and allosteric machines: new vistas and challenges for drug discovery

(2011) Terry P Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

Improving Drug Candidates by Design: A Focus on Physicochemical Properties As a Means of Improving Compound Disposition and Safety

(2011) Nicholas A. Meanwell   CHEMICAL RESEARCH IN TOXICOLOGY

Design Strategies for Bivalent Ligands Targeting GPCRs

(2011) Jeremy Shonberg et al.   ChemMedChem

What Do Medicinal Chemists Actually Make? A 50-Year Retrospective

(2011) W. Patrick Walters et al.   JOURNAL OF MEDICINAL CHEMISTRY

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

(2011) Bruce J. Melancon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the human histamine H1 receptor complex with doxepin

(2011) Tatsuro Shimamura et al.   NATURE

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Structure and function of an irreversible agonist-β2 adrenoceptor complex

(2011) Daniel M. Rosenbaum et al.   NATURE

Pathway and mechanism of drug binding to G-protein-coupled receptors

(2011) Ron O. Dror et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Allostery in pharmacology: Thermodynamics, evolution and design

(2011) Gábor Maksay   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

GPCR agonist binding revealed by modeling and crystallography

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Domain coupling in GPCRs: the engine for induced conformational changes

(2011) Hamiyet Unal et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Diversity and modularity of G protein-coupled receptor structures

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Molecular obesity, potency and other addictions in drug discovery

(2011) Michael M. Hann   MedChemComm

Allosteric Receptors: From Electric Organ to Cognition

(2010) Jean-Pierre Changeux   Annual Review of Pharmacology and Toxicology

Strategies for the identification of allosteric modulators of G-protein-coupled receptors

(2010) Neil T. Burford et al.   BIOCHEMICAL PHARMACOLOGY

Rational design of dualsteric GPCR ligands: quests and promise

(2010) Klaus Mohr et al.   BRITISH JOURNAL OF PHARMACOLOGY

Structural Determinants of Allosteric Agonism and Modulation at the M4Muscarinic Acetylcholine Receptor

(2010) Vindhya Nawaratne et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of Orthosteric and Allosteric Site Mutations in M2Muscarinic Acetylcholine Receptors That Contribute to Ligand-selective Signaling Bias

(2010) Karen J. Gregory et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hybrid Ortho/Allosteric Ligands for the Adenosine A1Receptor

(2010) Rajeshwar Narlawar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

(2010) Gregory J. Digby et al.   Molecular BioSystems

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation

(2010) M.C. Peeters et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors

(2009) Shijun Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Adenosine A2AReceptor-Antagonist/Dopamine D2Receptor-Agonist Bivalent Ligands as Pharmacological Tools to Detect A2A-D2Receptor Heteromers

(2009) Aroa Soriano et al.   JOURNAL OF MEDICINAL CHEMISTRY

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Cinacalcet – ein allosterischer Verstärker am Ca2+-Rezeptor

(2008) A Kebig et al.   DEUTSCHE MEDIZINISCHE WOCHENSCHRIFT

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity

(2008) Johannes Antony et al.   FASEB JOURNAL

A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity

(2008) Celine Valant et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE