Literature DB >> 26100629

Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily.

Bryan L Roth1, Wesley K Kroeze2.   

Abstract

G-protein-coupled receptors (GPCRs) are frequent and fruitful targets for drug discovery and development, as well as being off-targets for the side effects of a variety of medications. Much of the druggable non-olfactory human GPCR-ome remains under-interrogated, and we present here various approaches that we and others have used to shine light into these previously dark corners of the human genome.
© 2015 by The American Society for Biochemistry and Molecular Biology, Inc.

Entities:  

Keywords:  G-protein-coupled receptor (GPCR); chemical biology; cheminformatics; disease; druggable genome; functional genomics; molecular pharmacology; neurological disease

Mesh：

Substances：

Year:  2015        PMID： 26100629      PMCID： PMC4528112          DOI： 10.1074/jbc.R115.654764

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


  72 in total

1.  Identifying mechanism-of-action targets for drugs and probes.

Authors:  Elisabet Gregori-Puigjané; Vincent Setola; Jérôme Hert; Brenda A Crews; John J Irwin; Eugen Lounkine; Lawrence Marnett; Bryan L Roth; Brian K Shoichet
Journal:  Proc Natl Acad Sci U S A       Date:  2012-06-18       Impact factor: 11.205

Review 2.  Emerging paradigms in GPCR allostery: implications for drug discovery.

Authors:  Denise Wootten; Arthur Christopoulos; Patrick M Sexton
Journal:  Nat Rev Drug Discov       Date:  2013-08       Impact factor: 84.694

3.  Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.

Authors:  Xingyu Lin; Xi-Ping Huang; Gang Chen; Ryan Whaley; Shiming Peng; Yanli Wang; Guoliang Zhang; Simon X Wang; Shaohui Wang; Bryan L Roth; Niu Huang
Journal:  J Med Chem       Date:  2012-06-19       Impact factor: 7.446

4.  TGFα shedding assay: an accurate and versatile method for detecting GPCR activation.

Authors:  Asuka Inoue; Jun Ishiguro; Hajime Kitamura; Naoaki Arima; Michiyo Okutani; Akira Shuto; Shigeki Higashiyama; Tomohiko Ohwada; Hiroyuki Arai; Kumiko Makide; Junken Aoki
Journal:  Nat Methods       Date:  2012-09-16       Impact factor: 28.547

5.  Structure of the human smoothened receptor bound to an antitumour agent.

Authors:  Chong Wang; Huixian Wu; Vsevolod Katritch; Gye Won Han; Xi-Ping Huang; Wei Liu; Fai Yiu Siu; Bryan L Roth; Vadim Cherezov; Raymond C Stevens
Journal:  Nature       Date:  2013-05-01       Impact factor: 49.962

6.  Structural features for functional selectivity at serotonin receptors.

Authors:  Daniel Wacker; Chong Wang; Vsevolod Katritch; Gye Won Han; Xi-Ping Huang; Eyal Vardy; John D McCorvy; Yi Jiang; Meihua Chu; Fai Yiu Siu; Wei Liu; H Eric Xu; Vadim Cherezov; Bryan L Roth; Raymond C Stevens
Journal:  Science       Date:  2013-03-21       Impact factor: 47.728

7.  Structural basis for molecular recognition at serotonin receptors.

Authors:  Chong Wang; Yi Jiang; Jinming Ma; Huixian Wu; Daniel Wacker; Vsevolod Katritch; Gye Won Han; Wei Liu; Xi-Ping Huang; Eyal Vardy; John D McCorvy; Xiang Gao; X Edward Zhou; Karsten Melcher; Chenghai Zhang; Fang Bai; Huaiyu Yang; Linlin Yang; Hualiang Jiang; Bryan L Roth; Vadim Cherezov; Raymond C Stevens; H Eric Xu
Journal:  Science       Date:  2013-03-21       Impact factor: 47.728

8.  Automated design of ligands to polypharmacological profiles.

Authors:  Jérémy Besnard; Gian Filippo Ruda; Vincent Setola; Keren Abecassis; Ramona M Rodriguiz; Xi-Ping Huang; Suzanne Norval; Maria F Sassano; Antony I Shin; Lauren A Webster; Frederick R C Simeons; Laste Stojanovski; Annik Prat; Nabil G Seidah; Daniel B Constam; G Richard Bickerton; Kevin D Read; William C Wetsel; Ian H Gilbert; Bryan L Roth; Andrew L Hopkins
Journal:  Nature       Date:  2012-12-13       Impact factor: 49.962

9.  A pharmacological organization of G protein-coupled receptors.

Authors:  Henry Lin; Maria F Sassano; Bryan L Roth; Brian K Shoichet
Journal:  Nat Methods       Date:  2013-01-06       Impact factor: 28.547

10.  Conformation guides molecular efficacy in docking screens of activated β-2 adrenergic G protein coupled receptor.

Authors:  Dahlia R Weiss; SeungKirl Ahn; Maria F Sassano; Andrew Kleist; Xiao Zhu; Ryan Strachan; Bryan L Roth; Robert J Lefkowitz; Brian K Shoichet
Journal:  ACS Chem Biol       Date:  2013-03-21       Impact factor: 5.100
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  33 in total

1.  Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc.

Authors:  Seiji Sato; Xi-Ping Huang; Wesley K Kroeze; Bryan L Roth
Journal:  Mol Pharmacol       Date:  2016-10-17       Impact factor: 4.436

2.  A Pharmacochaperone-Based High-Throughput Screening Assay for the Discovery of Chemical Probes of Orphan Receptors.

Authors:  Camilo J Morfa; Daniel Bassoni; Andras Szabo; Danielle McAnally; Haleli Sharir; Becky L Hood; Stefan Vasile; Tom Wehrman; Jane Lamerdin; Layton H Smith
Journal:  Assay Drug Dev Technol       Date:  2018-09-22       Impact factor: 1.738

3.  A dynamic and screening-compatible nanoluciferase-based complementation assay enables profiling of individual GPCR-G protein interactions.

Authors:  Céline Laschet; Nadine Dupuis; Julien Hanson
Journal:  J Biol Chem       Date:  2018-12-28       Impact factor: 5.157

Review 4.  How Ligands Illuminate GPCR Molecular Pharmacology.

Authors:  Daniel Wacker; Raymond C Stevens; Bryan L Roth
Journal:  Cell       Date:  2017-07-27       Impact factor: 41.582

Review 5.  The current state of GPCR-based drug discovery to treat metabolic disease.

Authors:  Kyle W Sloop; Paul J Emmerson; Michael A Statnick; Francis S Willard
Journal:  Br J Pharmacol       Date:  2018-03-25       Impact factor: 8.739

Review 6.  What is new in pain modification in osteoarthritis?

Authors:  Rachel E Miller; Joel A Block; Anne-Marie Malfait
Journal:  Rheumatology (Oxford)       Date:  2018-05-01       Impact factor: 7.580

7.  Rare-variant pathogenicity triage and inclusion of synonymous variants improves analysis of disease associations of orphan G protein-coupled receptors.

Authors:  Ridge Dershem; Raghu P R Metpally; Kirk Jeffreys; Sarathbabu Krishnamurthy; Diane T Smelser; Michal Hershfinkel; David J Carey; Janet D Robishaw; Gerda E Breitwieser
Journal:  J Biol Chem       Date:  2019-10-18       Impact factor: 5.157

Review 8.  Neuro-psychopharmacological perspective of Orphan receptors of Rhodopsin (class A) family of G protein-coupled receptors.

Authors:  Muhammad Zahid Khan; Ling He
Journal:  Psychopharmacology (Berl)       Date:  2017-03-13       Impact factor: 4.530

9.  Target class drug discovery.

Authors:  Kimberly D Barnash; Lindsey I James; Stephen V Frye
Journal:  Nat Chem Biol       Date:  2017-09-19       Impact factor: 15.040

Review 10.  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
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