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

Chiemela S. Odoemelam, Benita Percival, Helen Wallis, Ming Wei Chang, Zeeshan Ahmad, Dawn Scholey, Emily Burton, Ian H. Williams, Caroline Lynn Kamerlin, Philippe B. Wilson

Research output: Contribution to journalReview article

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

Original languageEnglish
Pages (from-to)36337-36348
Number of pages12
JournalRSC Advances
Volume10
Issue number60
Early online date1 Oct 2020
DOIs
Publication statusPublished - 31 Oct 2020

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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