Literature DB >> 29394497

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

Kyle W Sloop1, Paul J Emmerson1, Michael A Statnick1, Francis S Willard2.   

Abstract

One approach of modern drug discovery is to identify agents that enhance or diminish signal transduction cascades in various cell types and tissues by modulating the activity of GPCRs. This strategy has resulted in the development of new medicines to treat many conditions, including cardiovascular disease, psychiatric disorders, HIV/AIDS, certain forms of cancer and Type 2 diabetes mellitus (T2DM). These successes justify further pursuit of GPCRs as disease targets and provide key learning that should help guide identifying future therapeutic agents. This report reviews the current landscape of GPCR drug discovery with emphasis on efforts aimed at developing new molecules for treating T2DM and obesity. We analyse historical efforts to generate GPCR-based drugs to treat metabolic disease in terms of causal factors leading to success and failure in this endeavour. LINKED ARTICLES: This article is part of a themed section on Molecular Pharmacology of GPCRs. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.21/issuetoc.
© 2018 The British Pharmacological Society.

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Year:  2018        PMID： 29394497      PMCID： PMC6177613          DOI： 10.1111/bph.14157

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  75 in total

Review 1.  Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily.

Authors:  Bryan L Roth; Wesley K Kroeze
Journal:  J Biol Chem       Date:  2015-06-22       Impact factor: 5.157

2.  Effects of JNJ-38431055, a novel GPR119 receptor agonist, in randomized, double-blind, placebo-controlled studies in subjects with type 2 diabetes.

Authors:  L B Katz; J J Gambale; P L Rothenberg; S R Vanapalli; N Vaccaro; L Xi; T C Sarich; P P Stein
Journal:  Diabetes Obes Metab       Date:  2012-03-14       Impact factor: 6.577

3.  THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein-coupled receptors.

Authors:  Stephen Ph Alexander; Arthur Christopoulos; Anthony P Davenport; Eamonn Kelly; Neil V Marrion; John A Peters; Elena Faccenda; Simon D Harding; Adam J Pawson; Joanna L Sharman; Christopher Southan; Jamie A Davies
Journal:  Br J Pharmacol       Date:  2017-12       Impact factor: 8.739

4.  The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling.

Authors:  Tingting Li; Sam R Holmstrom; Serkan Kir; Michihisa Umetani; Daniel R Schmidt; Steven A Kliewer; David J Mangelsdorf
Journal:  Mol Endocrinol       Date:  2011-03-31

5.  Safety, Pharmacokinetics, and Pharmacodynamic Effects of a Selective TGR5 Agonist, SB-756050, in Type 2 Diabetes.

Authors:  Rebecca J Hodge; Jiang Lin; Lakshmi S Vasist Johnson; Elizabeth P Gould; Gary D Bowers; Derek J Nunez
Journal:  Clin Pharmacol Drug Dev       Date:  2013-05-14

6.  Potent and selective agonism of the melanocortin receptor 4 with MK-0493 does not induce weight loss in obese human subjects: energy intake predicts lack of weight loss efficacy.

Authors:  R Krishna; B Gumbiner; C Stevens; B Musser; M Mallick; S Suryawanshi; L Maganti; H Zhu; T H Han; L Scherer; B Simpson; D Cosgrove; K Gottesdiener; J Amatruda; B J Rolls; J Blundell; G A Bray; K Fujioka; S B Heymsfield; J A Wagner; G A Herman
Journal:  Clin Pharmacol Ther       Date:  2009-09-09       Impact factor: 6.875

7.  Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease.

Authors:  Hong Lan; Lizbeth M Hoos; Li Liu; Glen Tetzloff; Weiwen Hu; Susan J Abbondanzo; Galya Vassileva; Eric L Gustafson; Joseph A Hedrick; Harry R Davis
Journal:  Diabetes       Date:  2008-08-04       Impact factor: 9.461

8.  Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial.

Authors:  K Kaku; K Enya; R Nakaya; T Ohira; R Matsuno
Journal:  Diabetes Obes Metab       Date:  2015-04-23       Impact factor: 6.577

9.  The IUPHAR/BPS Guide to PHARMACOLOGY in 2018: updates and expansion to encompass the new guide to IMMUNOPHARMACOLOGY.

Authors:  Simon D Harding; Joanna L Sharman; Elena Faccenda; Chris Southan; Adam J Pawson; Sam Ireland; Alasdair J G Gray; Liam Bruce; Stephen P H Alexander; Stephen Anderton; Clare Bryant; Anthony P Davenport; Christian Doerig; Doriano Fabbro; Francesca Levi-Schaffer; Michael Spedding; Jamie A Davies
Journal:  Nucleic Acids Res       Date:  2018-01-04       Impact factor: 16.971

10.  THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Nuclear hormone receptors.

Authors:  Stephen Ph Alexander; John A Cidlowski; Eamonn Kelly; Neil V Marrion; John A Peters; Elena Faccenda; Simon D Harding; Adam J Pawson; Joanna L Sharman; Christopher Southan; Jamie A Davies
Journal:  Br J Pharmacol       Date:  2017-12       Impact factor: 8.739
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  13 in total

1.  Molecular pharmacology of GPCRs.

Authors:  Christopher J Langmead; Roger J Summers
Journal:  Br J Pharmacol       Date:  2018-11       Impact factor: 8.739

2.  A Large Multiethnic Genome-Wide Association Study of Adult Body Mass Index Identifies Novel Loci.

Authors:  Thomas J Hoffmann; Hélène Choquet; Jie Yin; Yambazi Banda; Mark N Kvale; Maria Glymour; Catherine Schaefer; Neil Risch; Eric Jorgenson
Journal:  Genetics       Date:  2018-08-14       Impact factor: 4.562

Review 3.  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

4.  Effects of site-directed mutagenesis of GLP-1 and glucagon receptors on signal transduction activated by dual and triple agonists.

Authors:  Sanaz Darbalaei; Ru-Lue Chang; Qing-Tong Zhou; Yan Chen; An-Tao Dai; Ming-Wei Wang; De-Hua Yang
Journal:  Acta Pharmacol Sin       Date:  2022-08-11       Impact factor: 7.169

Review 5.  Cholesterol-dependent endocytosis of GPCRs: implications in pathophysiology and therapeutics.

Authors:  G Aditya Kumar; Amitabha Chattopadhyay
Journal:  Biophys Rev       Date:  2021-11-12

Review 6.  Multiscale Molecular Modeling in G Protein-Coupled Receptor (GPCR)-Ligand Studies.

Authors:  Pratanphorn Nakliang; Raudah Lazim; Hyerim Chang; Sun Choi
Journal:  Biomolecules       Date:  2020-04-19

Review 7.  Regulatory roles of G-protein coupled receptors in adipose tissue metabolism and their therapeutic potential.

Authors:  Hyeonyeong Im; Ji-Hyun Park; Seowoo Im; Juhyeong Han; Kyungmin Kim; Yun-Hee Lee
Journal:  Arch Pharm Res       Date:  2021-02-07       Impact factor: 4.946

8.  F2r negatively regulates osteoclastogenesis through inhibiting the Akt and NFκB signaling pathways.

Authors:  Yan Zhang; He Wang; Guochun Zhu; Airong Qian; Wei Chen
Journal:  Int J Biol Sci       Date:  2020-03-12       Impact factor: 6.580

9.  Characterizing Interhelical Interactions of G-Protein Coupled Receptors with the Fragment Molecular Orbital Method.

Authors:  Alexander Heifetz; Inaki Morao; M Madan Babu; Tim James; Michelle W Y Southey; Dmitri G Fedorov; Matteo Aldeghi; Michael J Bodkin; Andrea Townsend-Nicholson
Journal:  J Chem Theory Comput       Date:  2020-03-09       Impact factor: 6.006

10.  An activator of G protein-coupled receptor and MEK1/2-ERK1/2 signaling inhibits HIV-1 replication by altering viral RNA processing.

Authors:  Raymond W Wong; Ahalya Balachandran; Peter K Cheung; Ran Cheng; Qun Pan; Peter Stoilov; P Richard Harrigan; Benjamin J Blencowe; Donald R Branch; Alan Cochrane
Journal:  PLoS Pathog       Date:  2020-02-18       Impact factor: 6.823
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