Literature DB >> 26100628

From G Protein-coupled Receptor Structure Resolution to Rational Drug Design.

Ali Jazayeri1, Joao M Dias2, Fiona H Marshall2.   

Abstract

A number of recent technical solutions have led to significant advances in G protein-coupled receptor (GPCR) structural biology. Apart from a detailed mechanistic view of receptor activation, the new structures have revealed novel ligand binding sites. Together, these insights provide avenues for rational drug design to modulate the activities of these important drug targets. The application of structural data to GPCR drug discovery ushers in an exciting era with the potential to improve existing drugs and discover new ones. In this review, we focus on technical solutions that have accelerated GPCR crystallography as well as some of the salient findings from structures that are relevant to drug discovery. Finally, we outline some of the approaches used in GPCR structure based drug design.
© 2015 by The American Society for Biochemistry and Molecular Biology, Inc.

Entities:  

Keywords:  G protein-coupled receptor (GPCR); X-ray crystallography; drug design; drug discovery; membrane protein

Mesh：

Substances：

Year:  2015        PMID： 26100628      PMCID： PMC4528114          DOI： 10.1074/jbc.R115.668251

Source DB:  PubMed          Journal:  J Biol Chem        ISSN： 0021-9258            Impact factor:   5.157


  52 in total

Review 1.  Methodological advances: the unsung heroes of the GPCR structural revolution.

Authors:  Eshan Ghosh; Punita Kumari; Deepika Jaiman; Arun K Shukla
Journal:  Nat Rev Mol Cell Biol       Date:  2015-01-15       Impact factor: 94.444

2.  Structure of the human P2Y12 receptor in complex with an antithrombotic drug.

Authors:  Kaihua Zhang; Jin Zhang; Zhan-Guo Gao; Dandan Zhang; Lan Zhu; Gye Won Han; Steven M Moss; Silvia Paoletta; Evgeny Kiselev; Weizhen Lu; Gustavo Fenalti; Wenru Zhang; Christa E Müller; Huaiyu Yang; Hualiang Jiang; Vadim Cherezov; Vsevolod Katritch; Kenneth A Jacobson; Raymond C Stevens; Beili Wu; Qiang Zhao
Journal:  Nature       Date:  2014-03-23       Impact factor: 49.962

3.  Two disparate ligand-binding sites in the human P2Y1 receptor.

Authors:  Dandan Zhang; Zhan-Guo Gao; Kaihua Zhang; Evgeny Kiselev; Steven Crane; Jiang Wang; Silvia Paoletta; Cuiying Yi; Limin Ma; Wenru Zhang; Gye Won Han; Hong Liu; Vadim Cherezov; Vsevolod Katritch; Hualiang Jiang; Raymond C Stevens; Kenneth A Jacobson; Qiang Zhao; Beili Wu
Journal:  Nature       Date:  2015-03-30       Impact factor: 49.962

4.  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

5.  High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.

Authors:  Ankita Srivastava; Jason Yano; Yoshihiko Hirozane; Georgia Kefala; Franz Gruswitz; Gyorgy Snell; Weston Lane; Anthony Ivetac; Kathleen Aertgeerts; Jasmine Nguyen; Andy Jennings; Kengo Okada
Journal:  Nature       Date:  2014-07-20       Impact factor: 49.962

6.  Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant.

Authors:  Jie Yin; Juan Carlos Mobarec; Peter Kolb; Daniel M Rosenbaum
Journal:  Nature       Date:  2014-12-22       Impact factor: 49.962

7.  Structural Insights into the Dynamic Process of β2-Adrenergic Receptor Signaling.

Authors:  Aashish Manglik; Tae Hun Kim; Matthieu Masureel; Christian Altenbach; Zhongyu Yang; Daniel Hilger; Michael T Lerch; Tong Sun Kobilka; Foon Sun Thian; Wayne L Hubbell; R Scott Prosser; Brian K Kobilka
Journal:  Cell       Date:  2015-05-14       Impact factor: 41.582

8.  Structure of the Angiotensin receptor revealed by serial femtosecond crystallography.

Authors:  Haitao Zhang; Hamiyet Unal; Cornelius Gati; Gye Won Han; Wei Liu; Nadia A Zatsepin; Daniel James; Dingjie Wang; Garrett Nelson; Uwe Weierstall; Michael R Sawaya; Qingping Xu; Marc Messerschmidt; Garth J Williams; Sébastien Boutet; Oleksandr M Yefanov; Thomas A White; Chong Wang; Andrii Ishchenko; Kalyan C Tirupula; Russell Desnoyer; Jesse Coe; Chelsie E Conrad; Petra Fromme; Raymond C Stevens; Vsevolod Katritch; Sadashiva S Karnik; Vadim Cherezov
Journal:  Cell       Date:  2015-04-23       Impact factor: 41.582

Review 9.  Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.

Authors:  P Jeffrey Conn; Craig W Lindsley; Jens Meiler; Colleen M Niswender
Journal:  Nat Rev Drug Discov       Date:  2014-09       Impact factor: 84.694

10.  Agonist-bound structure of the human P2Y12 receptor.

Authors:  Jin Zhang; Kaihua Zhang; Zhan-Guo Gao; Silvia Paoletta; Dandan Zhang; Gye Won Han; Tingting Li; Limin Ma; Wenru Zhang; Christa E Müller; Huaiyu Yang; Hualiang Jiang; Vadim Cherezov; Vsevolod Katritch; Kenneth A Jacobson; Raymond C Stevens; Beili Wu; Qiang Zhao
Journal:  Nature       Date:  2014-05-01       Impact factor: 49.962
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  32 in total

Review 1.  Identifying ligands at orphan GPCRs: current status using structure-based approaches.

Authors:  Tony Ngo; Irina Kufareva; James Lj Coleman; Robert M Graham; Ruben Abagyan; Nicola J Smith
Journal:  Br J Pharmacol       Date:  2016-03-05       Impact factor: 8.739

2.  Prediction of Conformation Specific Thermostabilizing Mutations for Class A G Protein-Coupled Receptors.

Authors:  Suvamay Jana; Soumadwip Ghosh; Sanychen Muk; Benjamin Levy; Nagarajan Vaidehi
Journal:  J Chem Inf Model       Date:  2019-08-27       Impact factor: 4.956

3.  Photoaffinity Labeling of the Human A2A Adenosine Receptor and Cross-link Position Analysis by Mass Spectrometry.

Authors:  Hideyuki Muranaka; Takaki Momose; Chiaki Handa; Tomonaga Ozawa
Journal:  ACS Med Chem Lett       Date:  2017-05-17       Impact factor: 4.345

Review 4.  GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures.

Authors:  Ichio Shimada; Takumi Ueda; Yutaka Kofuku; Matthew T Eddy; Kurt Wüthrich
Journal:  Nat Rev Drug Discov       Date:  2018-11-09       Impact factor: 84.694

Review 5.  Thematic Minireview Series: New Directions in G Protein-coupled Receptor Pharmacology.

Authors:  Henrik G Dohlman
Journal:  J Biol Chem       Date:  2015-06-30       Impact factor: 5.157

6.  Structure-Based Design and Discovery of New M2 Receptor Agonists.

Authors:  Inbar Fish; Anne Stößel; Katrin Eitel; Celine Valant; Sabine Albold; Harald Huebner; Dorothee Möller; Mary J Clark; Roger K Sunahara; Arthur Christopoulos; Brian K Shoichet; Peter Gmeiner
Journal:  J Med Chem       Date:  2017-11-13       Impact factor: 7.446

7.  Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists.

Authors:  Dilip K Tosh; Antonella Ciancetta; Eugene Warnick; Steven Crane; Zhan-Guo Gao; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2016-12-09       Impact factor: 7.446

Review 8.  Leveraging allostery to improve G protein-coupled receptor (GPCR)-directed therapeutics: cannabinoid receptor 1 as discovery target.

Authors:  David R Janero; Ganesh A Thakur
Journal:  Expert Opin Drug Discov       Date:  2016-10-21       Impact factor: 6.098

Review 9.  Trends in GPCR drug discovery: new agents, targets and indications.

Authors:  Alexander S Hauser; Misty M Attwood; Mathias Rask-Andersen; Helgi B Schiöth; David E Gloriam
Journal:  Nat Rev Drug Discov       Date:  2017-10-27       Impact factor: 84.694

10.  Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.

Authors:  Karen J Gregory; Ranganadh Velagaleti; David M Thal; Ryan M Brady; Arthur Christopoulos; P Jeffrey Conn; David J Lapinsky
Journal:  ACS Chem Biol       Date:  2016-05-04       Impact factor: 5.100
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