Literature DB >> 33414387

G protein-coupled receptors: structure- and function-based drug discovery.

Dehua Yang1,2, Qingtong Zhou3, Viktorija Labroska1,4, Shanshan Qin5, Sanaz Darbalaei1,4, Yiran Wu5, Elita Yuliantie1,4, Linshan Xie5,6, Houchao Tao5, Jianjun Cheng5, Qing Liu1,2, Suwen Zhao5,6, Wenqing Shui7,8, Yi Jiang9, Ming-Wei Wang10,11,12,13,14,15.   

Abstract

As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design. We are eye-witnessing tremendous progresses made recently in the understanding of their structure-function relationships that facilitated drug development at an unprecedented pace. This article intends to provide a comprehensive overview of this important field to a broader readership that shares some common interests in drug discovery.

Entities:  

Mesh:

Substances:

Year:  2021        PMID: 33414387      PMCID: PMC7790836          DOI: 10.1038/s41392-020-00435-w

Source DB:  PubMed          Journal:  Signal Transduct Target Ther        ISSN: 2059-3635


  312 in total

1.  Allosteric modulation of the cannabinoid CB1 receptor.

Authors:  Martin R Price; Gemma L Baillie; Adèle Thomas; Lesley A Stevenson; Morag Easson; Richard Goodwin; Adèle McLean; Lorraine McIntosh; Gillian Goodwin; Glenn Walker; Paul Westwood; Julia Marrs; Fiona Thomson; Phillip Cowley; Arthur Christopoulos; Roger G Pertwee; Ruth A Ross
Journal:  Mol Pharmacol       Date:  2005-08-19       Impact factor: 4.436

2.  Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.

Authors:  Chris de Graaf; Albert J Kooistra; Henry F Vischer; Vsevolod Katritch; Martien Kuijer; Mitsunori Shiroishi; So Iwata; Tatsuro Shimamura; Raymond C Stevens; Iwan J P de Esch; Rob Leurs
Journal:  J Med Chem       Date:  2011-11-07       Impact factor: 7.446

3.  Competitive MS binding assays for dopamine D2 receptors employing spiperone as a native marker.

Authors:  Karin V Niessen; Georg Höfner; Klaus T Wanner
Journal:  Chembiochem       Date:  2005-10       Impact factor: 3.164

4.  Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways.

Authors:  Tarsis F Brust; Michael P Hayes; David L Roman; Kevin D Burris; Val J Watts
Journal:  J Pharmacol Exp Ther       Date:  2014-12-24       Impact factor: 4.030

5.  Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.

Authors:  Andrew S Doré; Krzysztof Okrasa; Jayesh C Patel; Maria Serrano-Vega; Kirstie Bennett; Robert M Cooke; James C Errey; Ali Jazayeri; Samir Khan; Ben Tehan; Malcolm Weir; Giselle R Wiggin; Fiona H Marshall
Journal:  Nature       Date:  2014-07-06       Impact factor: 49.962

6.  The G protein-biased κ-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo.

Authors:  Kate L White; J Elliott Robinson; Hu Zhu; Jeffrey F DiBerto; Prabhakar R Polepally; Jordan K Zjawiony; David E Nichols; C J Malanga; Bryan L Roth
Journal:  J Pharmacol Exp Ther       Date:  2014-10-15       Impact factor: 4.030

Review 7.  Cinacalcet: pharmacological and clinical aspects.

Authors:  Piergiorgio Messa; Carlo Alfieri; Brigida Brezzi
Journal:  Expert Opin Drug Metab Toxicol       Date:  2008-12       Impact factor: 4.481

8.  Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells.

Authors:  Didier Cussac; Elisa Boutet-Robinet; Marie-Christine Ailhaud; Adrian Newman-Tancredi; Jean-Claude Martel; Nathalie Danty; Isabelle Rauly-Lestienne
Journal:  Eur J Pharmacol       Date:  2008-07-30       Impact factor: 4.432

9.  An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor.

Authors:  Xiangyu Liu; Jonas Kaindl; Magdalena Korczynska; Anne Stößel; Daniela Dengler; Markus Stanek; Harald Hübner; Mary J Clark; Jake Mahoney; Rachel Ann Matt; Xinyu Xu; Kunio Hirata; Brian K Shoichet; Roger K Sunahara; Brian K Kobilka; Peter Gmeiner
Journal:  Nat Chem Biol       Date:  2020-06-01       Impact factor: 15.040

10.  Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries.

Authors:  Seungkirl Ahn; Biswaranjan Pani; Alem W Kahsai; Eva K Olsen; Gitte Husemoen; Mikkel Vestergaard; Lei Jin; Shuai Zhao; Laura M Wingler; Paula K Rambarat; Rishabh K Simhal; Thomas T Xu; Lillian D Sun; Paul J Shim; Dean P Staus; Li-Yin Huang; Thomas Franch; Xin Chen; Robert J Lefkowitz
Journal:  Mol Pharmacol       Date:  2018-05-16       Impact factor: 4.436

View more
  30 in total

Review 1.  Cation-π Interactions and their Functional Roles in Membrane Proteins.

Authors:  Daniel T Infield; Ali Rasouli; Grace D Galles; Christophe Chipot; Emad Tajkhorshid; Christopher A Ahern
Journal:  J Mol Biol       Date:  2021-05-04       Impact factor: 5.469

Review 2.  AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors.

Authors:  Xin-Heng He; Chong-Zhao You; Hua-Liang Jiang; Yi Jiang; H Eric Xu; Xi Cheng
Journal:  Acta Pharmacol Sin       Date:  2022-07-01       Impact factor: 6.150

3.  Candidate Therapeutics by Screening for Multitargeting Ligands: Combining the CB2 Receptor With CB1, PPARγ and 5-HT4 Receptors.

Authors:  Shayma El-Atawneh; Amiram Goldblum
Journal:  Front Pharmacol       Date:  2022-02-28       Impact factor: 5.810

Review 4.  Pathophysiological impact of the adhesion G protein-coupled receptor family.

Authors:  Jeanette M Einspahr; Douglas G Tilley
Journal:  Am J Physiol Cell Physiol       Date:  2022-07-18       Impact factor: 5.282

Review 5.  Application of Mathematical Modeling and Computational Tools in the Modern Drug Design and Development Process.

Authors:  Md Rifat Hasan; Ahad Amer Alsaiari; Burhan Zain Fakhurji; Mohammad Habibur Rahman Molla; Amer H Asseri; Md Afsar Ahmed Sumon; Moon Nyeo Park; Foysal Ahammad; Bonglee Kim
Journal:  Molecules       Date:  2022-06-29       Impact factor: 4.927

6.  IBD-associated G protein-coupled receptor 65 variant compromises signalling and impairs key functions involved in inflammation.

Authors:  Virginie Mercier; Gabrielle Boucher; Dominic Devost; Kyla Bourque; Azadeh Alikashani; Claudine Beauchamp; Alain Bitton; Sylvain Foisy; Philippe Goyette; Guy Charron; Terence E Hébert; John D Rioux
Journal:  Cell Signal       Date:  2022-02-24       Impact factor: 4.850

7.  Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism.

Authors:  Zhenmei Xu; Tatsuya Ikuta; Kouki Kawakami; Ryoji Kise; Yu Qian; Ruixue Xia; Ming-Xia Sun; Anqi Zhang; Changyou Guo; Xue-Hui Cai; Zhiwei Huang; Asuka Inoue; Yuanzheng He
Journal:  Nat Chem Biol       Date:  2021-12-22       Impact factor: 16.174

8.  Cholesterol in GPCR Structures: Prevalence and Relevance.

Authors:  Parijat Sarkar; Amitabha Chattopadhyay
Journal:  J Membr Biol       Date:  2021-08-07       Impact factor: 1.843

Review 9.  Insights into Nuclear G-Protein-Coupled Receptors as Therapeutic Targets in Non-Communicable Diseases.

Authors:  Salomé Gonçalves-Monteiro; Rita Ribeiro-Oliveira; Maria Sofia Vieira-Rocha; Martin Vojtek; Joana B Sousa; Carmen Diniz
Journal:  Pharmaceuticals (Basel)       Date:  2021-05-07

Review 10.  G-Protein Coupled Receptors (GPCRs): Signaling Pathways, Characterization, and Functions in Insect Physiology and Toxicology.

Authors:  Nannan Liu; Yifan Wang; Ting Li; Xuechun Feng
Journal:  Int J Mol Sci       Date:  2021-05-17       Impact factor: 5.923

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.