Issue 60, 2020

G-Protein coupled receptors: structure and function in drug discovery

Abstract

The G-protein coupled receptors (GPCRs) superfamily comprise similar proteins arranged into families or classes thus making it one of the largest in the mammalian genome. GPCRs take part in many vital physiological functions making them targets for numerous novel drugs. GPCRs share some distinctive features, such as the seven transmembrane domains, they also differ in the number of conserved residues in their transmembrane domain. Here we provide an introductory and accessible review detailing the computational advances in GPCR pharmacology and drug discovery. An overview is provided on family A-C GPCRs; their structural differences, GPCR signalling, allosteric binding and cooperativity. The dielectric constant (relative permittivity) of proteins is also discussed in the context of site-specific environmental effects.

Graphical abstract: G-Protein coupled receptors: structure and function in drug discovery

Article information

Article type
Review Article
Submitted
20 iyl 2020
Accepted
22 sen 2020
First published
01 okt 2020
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2020,10, 36337-36348

G-Protein coupled receptors: structure and function in drug discovery

C. S. Odoemelam, B. Percival, H. Wallis, M. Chang, Z. Ahmad, D. Scholey, E. Burton, I. H. Williams, C. L. Kamerlin and P. B. Wilson, RSC Adv., 2020, 10, 36337 DOI: 10.1039/D0RA08003A

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. You can use material from this article in other publications, without requesting further permission from the RSC, provided that the correct acknowledgement is given and it is not used for commercial purposes.

To request permission to reproduce material from this article in a commercial publication, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party commercial publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements