Multiple Binding Sites Contribute to the Mechanism of Mixed Agonistic and Positive Allosteric Modulators of the Cannabinoid CB1 Receptor

An Efficient Metadynamics-Based Protocol To Model the Binding Affinity and the Transition State Ensemble of G-Protein-Coupled Receptor Ligands

(2017) Noureldin Saleh et al.   Journal of Chemical Information and Modeling

Structure of the full-length glucagon class B G-protein-coupled receptor

(2017) Haonan Zhang et al.   NATURE

Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators

(2017) Gaojie Song et al.   NATURE

Crystal structures of agonist-bound human cannabinoid receptor CB1

(2017) Tian Hua et al.   NATURE

Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities

(2017) Leepakshi Khurana et al.   NEUROPHARMACOLOGY

Investigating allosteric effects on the functional dynamics of β2-adrenergic ternary complexes with enhanced-sampling simulations

(2017) Noureldin Saleh et al.   Chemical Science

Identification of Two Distinct Sites for Antagonist and Biased Agonist Binding to the Human Chemokine Receptor CXCR3

(2016) Lampros Milanos et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Three-Site Mechanism for Agonist/Antagonist Selective Binding to Vasopressin Receptors

(2016) Noureldin Saleh et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

(2016) Yi Zheng et al.   NATURE

High-resolution crystal structure of the human CB1 cannabinoid receptor

(2016) Zhenhua Shao et al.   NATURE

Extra-helical binding site of a glucagon receptor antagonist

(2016) Ali Jazayeri et al.   NATURE

Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)

(2015) John A. Christopher et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects

(2015) Bogna M Ignatowska-Jankowska et al.   NEUROPSYCHOPHARMACOLOGY

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

(2014) Andrew S. Doré et al.   NATURE

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

(2014) H. Wu et al.   SCIENCE

Modulating the endocannabinoid system in human health and disease - successes and failures

(2013) Pál Pacher et al.   FEBS Journal

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Emerging paradigms in GPCR allostery: implications for drug discovery

(2013) Denise Wootten et al.   NATURE REVIEWS DRUG DISCOVERY

Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

(2013) Q. Tan et al.   SCIENCE

Biomolecular Simulation: A Computational Microscope for Molecular Biology

(2012) Ron O. Dror et al.   Annual Review of Biophysics

Cannabinoid-1 receptor (CB1R) blockers as medicines: beyond obesity and cardiometabolic disorders to substance abuse/drug addiction with CB1R neutral antagonists

(2012) David R. Janero   EXPERT OPINION ON EMERGING DRUGS

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

(2012) Andreas Bock et al.   Nature Communications

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2

(2010) R. G. Pertwee et al.   PHARMACOLOGICAL REVIEWS

Latest advances in cannabinoid receptor agonists

(2009) Ganesh A Thakur et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Ligands that target cannabinoid receptors in the brain: from THC to anandamide and beyond

(2008) Roger G. Pertwee   ADDICTION BIOLOGY

CB1 receptor antagonism: biological basis for metabolic effects

(2008) Vincenzo Di Marzo   DRUG DISCOVERY TODAY

Targeting the endocannabinoid system: to enhance or reduce?

(2008) Vincenzo Di Marzo   NATURE REVIEWS DRUG DISCOVERY

Pharmacotherapeutic targeting of the endocannabinoid signaling system: Drugs for obesity and the metabolic syndrome

(2007) V. Kiran Vemuri et al.   PHYSIOLOGY & BEHAVIOR