Crystal Structure of the Human Cannabinoid Receptor CB2.
Tian Hua,Kiran Vemuri,Mengchen Pu,Lu Qu,Lu Qu,Gye Won Han,Yiran Wu,Suwen Zhao,Wenqing Shui,Shanshan Li,Anisha Korde,Robert B. Laprairie,Edward L. Stahl,Jo-Hao Ho,Nikolai Zvonok,Han Zhou,Irina Kufareva,Beili Wu,Qiang Zhao,Michael A. Hanson,Laura M. Bohn,Alexandros Makriyannis,Raymond C. Stevens,Raymond C. Stevens,Zhi-Jie Liu,Zhi-Jie Liu +25 more
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TLDR
The structure of the CB1-AM6538 complex reveals key features of the receptor and critical interactions for antagonist binding and provides insight into the binding mode of naturally occurring CB1 ligands, such as THC, and synthetic cannabinoids.About:
This article is published in Cell.The article was published on 2016-10-20 and is currently open access. It has received 488 citations till now. The article focuses on the topics: Cannabinoid receptor type 2 & Cannabinoid receptor.read more
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Hepatic stellate cells as key target in liver fibrosis
TL;DR: Cell type- and target-specific pharmacological intervention to therapeutically induce the deactivation of hepatic stellate cells will enable more effective and less toxic precision antifibrotic therapies.
Journal ArticleDOI
Cannabinoid Receptors and the Endocannabinoid System: Signaling and Function in the Central Nervous System.
Shenglong Zou,Ujendra Kumar +1 more
TL;DR: It is believed that the therapeutic significance of cannabinoids is masked by the adverse effects and here alternative strategies are discussed to take therapeutic advantage of cannabinoids.
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3D Variability Analysis: Resolving continuous flexibility and discrete heterogeneity from single particle cryo-EM.
Ali Punjani,David J. Fleet +1 more
TL;DR: 3D variability analysis (3DVA) as discussed by the authors fits a linear subspace model of conformational change to cryo-EM data at high resolution, enabling the resolution and visualization of detailed molecular motions of both large and small proteins.
Journal ArticleDOI
How Ligands Illuminate GPCR Molecular Pharmacology.
TL;DR: Structural and molecular insights into ligand engagement and action have enabled new computational methods and accelerated the discovery of novel ligands and tool compounds, especially for understudied andorphan GPCRs, and promise to streamline the development of GPCR-targeted medications.
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Crystal structures of agonist-bound human cannabinoid receptor CB1
Tian Hua,Kiran Vemuri,Spyros P. Nikas,Robert B. Laprairie,Yiran Wu,Lu Qu,Lu Qu,Mengchen Pu,Anisha Korde,Shan Jiang,Jo-Hao Ho,Gye Won Han,Kang Ding,Kang Ding,Xuanxuan Li,Haiguang Liu,Michael A. Hanson,Suwen Zhao,Laura M. Bohn,Alexandros Makriyannis,Raymond C. Stevens,Raymond C. Stevens,Zhi-Jie Liu,Zhi-Jie Liu +23 more
TL;DR: The structures reveal important insights into the activation mechanism of CB1 and provide a molecular basis for predicting the binding modes of Δ9-THC, and endogenous and synthetic cannabinoids and should inspire the design of chemically diverse ligands with distinct pharmacological properties.
References
More filters
Journal ArticleDOI
MAFFT Multiple Sequence Alignment Software Version 7: Improvements in Performance and Usability
Kazutaka Katoh,Daron M. Standley +1 more
TL;DR: This version of MAFFT has several new features, including options for adding unaligned sequences into an existing alignment, adjustment of direction in nucleotide alignment, constrained alignment and parallel processing, which were implemented after the previous major update.
Journal ArticleDOI
Features and development of Coot.
TL;DR: Coot is a molecular-graphics program designed to assist in the building of protein and other macromolecular models and the current state of development and available features are presented.
Journal ArticleDOI
PHENIX: a comprehensive Python-based system for macromolecular structure solution
Paul D. Adams,Paul D. Adams,Pavel V. Afonine,Gábor Bunkóczi,Vincent B. Chen,Ian W. Davis,Nathaniel Echols,Jeffrey J. Headd,Li-Wei Hung,Gary J. Kapral,Ralf W. Grosse-Kunstleve,Airlie J. McCoy,Nigel W. Moriarty,Robert D. Oeffner,Randy J. Read,David S. Richardson,Jane S. Richardson,Thomas C. Terwilliger,Peter H. Zwart +18 more
TL;DR: The PHENIX software for macromolecular structure determination is described and its uses and benefits are described.
Journal ArticleDOI
Phaser crystallographic software
Airlie J. McCoy,Ralf W. Grosse-Kunstleve,Paul D. Adams,Martyn Winn,Laurent C. Storoni,Randy J. Read +5 more
TL;DR: A description is given of Phaser-2.1: software for phasing macromolecular crystal structures by molecular replacement and single-wavelength anomalous dispersion phasing.
Journal ArticleDOI
The CCP4 suite: programs for protein crystallography
TL;DR: The CCP4 (Collaborative Computational Project, number 4) program suite is a collection of programs and associated data and subroutine libraries which can be used for macromolecular structure determination by X-ray crystallography.