Literature DB >> 24628305

Structure of Class B GPCRs: new horizons for drug discovery.

Andrea Bortolato1, Andrew S Doré, Kaspar Hollenstein, Benjamin G Tehan, Jonathan S Mason, Fiona H Marshall.   

Abstract

Class B GPCRs of the secretin family are important drug targets in many human diseases including diabetes, neurodegeneration, cardiovascular disease and psychiatric disorders. X-ray crystal structures for the glucagon receptor and corticotropin-releasing factor receptor 1 have now been published. In this review, we analyse the new structures and how they compare with each other and with Class A and F receptors. We also consider the differences in druggability and possible similarity in the activation mechanisms. Finally, we discuss the potential for the design of small-molecule modulators for these important targets in drug discovery. This new structural insight allows, for the first time, structure-based drug design methods to be applied to Class B GPCRs.
© 2014 The British Pharmacological Society.

Entities:  

Keywords:  CRF1 receptor; Class B; GPCR; GPCR molecular signature; HHM; druggability; glucagon receptor; smoothened receptor

Mesh：

Substances：

Year:  2014        PMID： 24628305      PMCID： PMC4080969          DOI： 10.1111/bph.12689

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


  51 in total

Review 1.  New insights from structural biology into the druggability of G protein-coupled receptors.

Authors:  Jonathan S Mason; Andrea Bortolato; Miles Congreve; Fiona H Marshall
Journal:  Trends Pharmacol Sci       Date:  2012-03-30       Impact factor: 14.819

Review 2.  Drugability of extracellular targets: discovery of small molecule drugs targeting allosteric, functional, and subunit-selective sites on GPCRs and ion channels.

Authors:  Dimitri E Grigoriadis; Samuel R J Hoare; Sandra M Lechner; Deborah H Slee; John A Williams
Journal:  Neuropsychopharmacology       Date:  2008-09-17       Impact factor: 7.853

Review 3.  The use of GPCR structures in drug design.

Authors:  Miles Congreve; Christopher Langmead; Fiona H Marshall
Journal:  Adv Pharmacol       Date:  2011

4.  Molecular basis for negative regulation of the glucagon receptor.

Authors:  Christopher M Koth; Jeremy M Murray; Susmith Mukund; Azadeh Madjidi; Alexandra Minn; Holly J Clarke; Terence Wong; Vicki Chiang; Elizabeth Luis; Alberto Estevez; Jesus Rondon; Yingnan Zhang; Isidro Hötzel; Bernard B Allan
Journal:  Proc Natl Acad Sci U S A       Date:  2012-08-20       Impact factor: 11.205

5.  Small-molecule agonists for the glucagon-like peptide 1 receptor.

Authors:  Lotte Bjerre Knudsen; Dan Kiel; Min Teng; Carsten Behrens; Dilip Bhumralkar; János T Kodra; Jens J Holst; Claus B Jeppesen; Michael D Johnson; Johannes Cornelis de Jong; Anker Steen Jorgensen; Tim Kercher; Jarek Kostrowicki; Peter Madsen; Preben H Olesen; Jacob S Petersen; Fritz Poulsen; Ulla G Sidelmann; Jeppe Sturis; Larry Truesdale; John May; Jesper Lau
Journal:  Proc Natl Acad Sci U S A       Date:  2007-01-09       Impact factor: 11.205

6.  A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.

Authors:  Desu Chen; Jiayu Liao; Na Li; Caihong Zhou; Qing Liu; Guangxing Wang; Rui Zhang; Song Zhang; Lilin Lin; Kaixian Chen; Xin Xie; Fajun Nan; Andrew A Young; Ming-Wei Wang
Journal:  Proc Natl Acad Sci U S A       Date:  2007-01-09       Impact factor: 11.205

Review 7.  Insights into the structure of class B GPCRs.

Authors:  Kaspar Hollenstein; Chris de Graaf; Andrea Bortolato; Ming-Wei Wang; Fiona H Marshall; Raymond C Stevens
Journal:  Trends Pharmacol Sci       Date:  2013-12-18       Impact factor: 14.819

8.  Structure-based discovery of allosteric modulators of two related class B G-protein-coupled receptors.

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Journal:  ChemMedChem       Date:  2011-10-12       Impact factor: 3.466

9.  The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints.

Authors:  Robert Fredriksson; Malin C Lagerström; Lars-Gustav Lundin; Helgi B Schiöth
Journal:  Mol Pharmacol       Date:  2003-06       Impact factor: 4.436

10.  Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.

Authors:  Miles Congreve; Stephen P Andrews; Andrew S Doré; Kaspar Hollenstein; Edward Hurrell; Christopher J Langmead; Jonathan S Mason; Irene W Ng; Benjamin Tehan; Andrei Zhukov; Malcolm Weir; Fiona H Marshall
Journal:  J Med Chem       Date:  2012-01-27       Impact factor: 7.446
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  33 in total

1.  Fluorescent bioorthogonal labeling of class B GPCRs in live cells.

Authors:  Srikanth Kumar Gangam; Qing Lin
Journal:  Methods Enzymol       Date:  2020-06-15       Impact factor: 1.600

Review 2.  Structural insights into ligand recognition and selectivity for classes A, B, and C GPCRs.

Authors:  Sang-Min Lee; Jason M Booe; Augen A Pioszak
Journal:  Eur J Pharmacol       Date:  2015-05-14       Impact factor: 4.432

Review 3.  Novel Allosteric Modulators of G Protein-coupled Receptors.

Authors:  Patrick R Gentry; Patrick M Sexton; Arthur Christopoulos
Journal:  J Biol Chem       Date:  2015-06-22       Impact factor: 5.157

4.  Actions of the small molecule ligands SW106 and AH-3960 on the type-1 parathyroid hormone receptor.

Authors:  Percy H Carter; Thomas Dean; Brijesh Bhayana; Ashok Khatri; Raj Rajur; Thomas J Gardella
Journal:  Mol Endocrinol       Date:  2015-01-13

5.  Activation of the GLP-1 receptor by a non-peptidic agonist.

Authors:  Peishen Zhao; Yi-Lynn Liang; Matthew J Belousoff; Giuseppe Deganutti; Madeleine M Fletcher; Francis S Willard; Michael G Bell; Michael E Christe; Kyle W Sloop; Asuka Inoue; Tin T Truong; Lachlan Clydesdale; Sebastian G B Furness; Arthur Christopoulos; Ming-Wei Wang; Laurence J Miller; Christopher A Reynolds; Radostin Danev; Patrick M Sexton; Denise Wootten
Journal:  Nature       Date:  2020-01-08       Impact factor: 49.962

Review 6.  Structural Basis for Allosteric Modulation of Class B G Protein-Coupled Receptors.

Authors:  Denise Wootten; Laurence J Miller
Journal:  Annu Rev Pharmacol Toxicol       Date:  2019-08-27       Impact factor: 13.820

7.  G-Protein-Coupled Receptor SRBC-48 Protects against Dendrite Degeneration and Reduced Longevity Due to Infection.

Authors:  Supender Kaur; Alejandro Aballay
Journal:  Cell Rep       Date:  2020-05-19       Impact factor: 9.423

Review 8.  Incretin drugs in diabetic kidney disease: biological mechanisms and clinical evidence.

Authors:  Radica Z Alicic; Emily J Cox; Joshua J Neumiller; Katherine R Tuttle
Journal:  Nat Rev Nephrol       Date:  2020-11-20       Impact factor: 28.314

9.  Development of Potent, Protease-Resistant Agonists of the Parathyroid Hormone Receptor with Broad β Residue Distribution.

Authors:  Ross W Cheloha; Bingming Chen; Niyanta N Kumar; Tomoyuki Watanabe; Robert G Thorne; Lingjun Li; Thomas J Gardella; Samuel H Gellman
Journal:  J Med Chem       Date:  2017-10-24       Impact factor: 7.446

10.  Differential Requirement of the Extracellular Domain in Activation of Class B G Protein-coupled Receptors.

Authors:  Li-Hua Zhao; Yanting Yin; Dehua Yang; Bo Liu; Li Hou; Xiaoxi Wang; Kuntal Pal; Yi Jiang; Yang Feng; Xiaoqing Cai; Antao Dai; Mingyao Liu; Ming-Wei Wang; Karsten Melcher; H Eric Xu
Journal:  J Biol Chem       Date:  2016-05-13       Impact factor: 5.157
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