4.4 Review

Structural and functional insights into the G protein-coupled receptors: CB1 and CB2

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Multidisciplinary Sciences

Structural basis for activation of CB1 by an endocannabinoid analog

Kaavya Krishna Kumar et al.

Summary: Understanding the structure and function of the interaction between endocannabinoids (eCBs) and cannabinoid receptor 1 (CB1) is important for developing effective drugs targeting this receptor. In this study, the structure of the AMG315-bound CB1 signaling complex was determined, revealing differences in the ligand binding pocket compared to previous structures. The functional consequences of ligand interactions with specific residues were investigated, and it was found that intracellular rearrangements in the TM2 region are unique to CB1 and play a role in G protein activation. Additionally, a CB1-specific allosteric modulator exploits this activation mechanism.

NATURE COMMUNICATIONS (2023)

Article Multidisciplinary Sciences

Structural basis of selective cannabinoid CB2 receptor activation

Xiaoting Li et al.

Summary: In this study, the authors report the discovery of a CB2R agonist, LEI-102, and investigate its selective activation of CB2R in conjunction with three other CBR ligands (APD371, HU308, and CP55,940). They identify key residues for CB2R activation and reveal the important role of lipophilicity in CB2R engagement. The favorable physico-chemical properties of LEI-102 enable its oral efficacy in a chemotherapy-induced nephropathy model.

NATURE COMMUNICATIONS (2023)

Article Biochemistry & Molecular Biology

Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1

Xin Yang et al.

Summary: This study presents the crystallographic and cryo-electron microscopy structures of CB1 receptor bound to the allosteric modulator ZCZ011. The results show that ZCZ011 induces rearrangement of TM2, promoting receptor activation and increasing the population of active receptors. In contrast, the negative allosteric modulator ORG27569 inhibits TM2 rearrangement. These findings provide insights into CB1 allosteric regulation and have implications for the rational design of allosteric modulators.

NATURE CHEMICAL BIOLOGY (2022)

Article Chemistry, Multidisciplinary

A Genetically Encoded F-19 NMR Probe Reveals the Allosteric Modulation Mechanism of Cannabinoid Receptor 1

Xiaoyan Wang et al.

Summary: A method for genetic incorporation of an unnatural amino acid into a cannabinoid receptor has been developed, revealing a previously unrecognized pre-active state through F-19 NMR and X-ray crystallography methods. An allosteric modulation model is proposed to explain the distinct behavior of the allosteric modulator Org27569. This site-specific F-19 NMR labeling method is a powerful tool for decoding the mechanism of GPCR allosteric modulation.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

Article Biochemistry & Molecular Biology

Cryo-EM Structure of the Human Cannabinoid Receptor CB2-Gi Signaling Complex

Changrui Xing et al.

Article Biochemistry & Molecular Biology

Molecular switches in GPCRs

Slawomir Filipek

CURRENT OPINION IN STRUCTURAL BIOLOGY (2019)

Article Pharmacology & Pharmacy

Cannabinoid CB1 and CB2 Receptor-Mediated Arrestin Translocation: Species, Subtype, and Agonist-Dependence

Mikkel Soes Ibsen et al.

FRONTIERS IN PHARMACOLOGY (2019)

Review Biochemistry & Molecular Biology

Cannabinoid Receptor Interacting Protein 1a (CRIP1a): Function and Structure

William T. Booth et al.

MOLECULES (2019)

Article Biochemistry & Molecular Biology

Structure of an allosteric modulator bound to the CB1 cannabinoid receptor

Zhenhua Shao et al.

NATURE CHEMICAL BIOLOGY (2019)

Article Biochemistry & Molecular Biology

Crystal Structure of the Human Cannabinoid Receptor CB2

Xiaoting Li et al.

Article Biochemistry & Molecular Biology

Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex

Kaavya Krishna Kumar et al.

Article Neurosciences

Rimonabant, a potent CB1 cannabinoid receptor antagonist, is a Gαi/o protein inhibitor

Alessandra Porcu et al.

NEUROPHARMACOLOGY (2018)

Article Multidisciplinary Sciences

Cryo-EM structure of human rhodopsin bound to an inhibitory G protein

Yanyong Kang et al.

NATURE (2018)

Article Multidisciplinary Sciences

Crystal structures of agonist-bound human cannabinoid receptor CB1

Tian Hua et al.

NATURE (2017)

Editorial Material Neurosciences

Editorial: The CB2 Cannabinoid System: A New Strategy in Neurodegenerative Disorder and Neuroinflammation

Marialessandra Contino et al.

FRONTIERS IN NEUROSCIENCE (2017)

Article Biochemistry & Molecular Biology

Crystal Structure of the Human Cannabinoid Receptor CB1

Tian Hua et al.

Article Multidisciplinary Sciences

High-resolution crystal structure of the human CB1 cannabinoid receptor

Zhenhua Shao et al.

NATURE (2016)

Article Multidisciplinary Sciences

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

David M. Thal et al.

NATURE (2016)

Article Biochemistry & Molecular Biology

Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1

Jill E. Chrencik et al.

Review Endocrinology & Metabolism

The Endocannabinoid System: Pivotal Orchestrator of Obesity and Metabolic Disease

Wilfrid Mazier et al.

TRENDS IN ENDOCRINOLOGY AND METABOLISM (2015)

Review Pharmacology & Pharmacy

Endocannabinoid signaling at the periphery: 50 years after THC

Mauro Maccarrone et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2015)

Article Multidisciplinary Sciences

Pregnenolone Can Protect the Brain from Cannabis Intoxication

Monique Vallee et al.

SCIENCE (2014)

Article Gastroenterology & Hepatology

Cannabinoid signaling and liver therapeutics

Ariane Mallat et al.

JOURNAL OF HEPATOLOGY (2013)

Article Multidisciplinary Sciences

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Andrew C. Kruse et al.

NATURE (2013)

Article Multidisciplinary Sciences

Structure of the agonist-bound neurotensin receptor

Jim F. White et al.

NATURE (2012)

Article Multidisciplinary Sciences

Structure and dynamics of the M3 muscarinic acetylcholine receptor

Andrew C. Kruse et al.

NATURE (2012)

Article Multidisciplinary Sciences

Crystal Structure of a Lipid G Protein-Coupled Receptor

Michael A. Hanson et al.

SCIENCE (2012)

Article Pharmacology & Pharmacy

Cannabinoid CB1 receptor ligand binding and function examined through mutagenesis studies of F200 and S383

Doree F. Sitkoff et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2011)

Article Biochemistry & Molecular Biology

Modeling of ligand binding to G protein coupled receptors: cannabinoid CB1, CB2 and adrenergic β2AR

Dorota Latek et al.

JOURNAL OF MOLECULAR MODELING (2011)

Article Biochemistry & Molecular Biology

A Lipid Pathway for Ligand Binding Is Necessary for a Cannabinoid G Protein-coupled Receptor

Dow P. Hurst et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2010)

Article Biophysics

Transmembrane Helical Domain of the Cannabinoid CB1 Receptor

Joong-Youn Shim

BIOPHYSICAL JOURNAL (2009)

Review Pharmacology & Pharmacy

Cannabinoid CB2 receptors: a therapeutic target for the treatment of inflammatory and neuropathic pain

J. Guindon et al.

BRITISH JOURNAL OF PHARMACOLOGY (2008)

Review Pharmacology & Pharmacy

Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists

C. A. Lunn et al.

BRITISH JOURNAL OF PHARMACOLOGY (2008)

Review Biochemistry & Molecular Biology

Lipid-mediated dimerization of β2-adrenergic receptor reveals important clues for cannabinoid receptors

E. Dainese et al.

CELLULAR AND MOLECULAR LIFE SCIENCES (2008)

Article Pharmacology & Pharmacy

CB1 cannabinoid receptor activity is modulated by the cannabinoid receptor interacting protein CRIP 1a

Jason L. Niehaus et al.

MOLECULAR PHARMACOLOGY (2007)

Article Chemistry, Medicinal

GPCR structure-based virtual screening approach for CB2 antagonist search

Jian-Zhong Chen et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2007)

Article Chemistry, Medicinal

WIN55212-2 docking to the CB1 cannabinoid receptor and multiple pathways for conformational induction

JY Shim et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2006)

Article Chemistry, Medicinal

Cannabinoid CB2/CB1 selectivity. Receptor modeling and automated docking analysis

T Tuccinardi et al.

JOURNAL OF MEDICINAL CHEMISTRY (2006)

Article Chemistry, Medicinal

Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor

OMH Salo et al.

JOURNAL OF MEDICINAL CHEMISTRY (2005)

Article Multidisciplinary Sciences

Identification and functional characterization of brainstem cannabinoid CB2 receptors

MD Van Sickle et al.

SCIENCE (2005)

Article Chemistry, Medicinal

Homology models of the cannabinoid CB1 and CB2 receptors. A docking analysis study

C Montero et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2005)

Review Neurosciences

The endogenous cannabinoid system and its role in nociceptive behavior

BF Cravatt et al.

JOURNAL OF NEUROBIOLOGY (2004)

Article Chemistry, Medicinal

Development of a 3D model for the human cannabinoid CB1 receptor

OMH Salo et al.

JOURNAL OF MEDICINAL CHEMISTRY (2004)

Article Biochemistry & Molecular Biology

3D structural model of the G-protein-coupled cannabinoid CB2 receptor

XQ Xie et al.

PROTEINS-STRUCTURE FUNCTION AND GENETICS (2003)

Article Pharmacology & Pharmacy

Cannabinoids and multiple sclerosis

RG Pertwee

PHARMACOLOGY & THERAPEUTICS (2002)