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Structure‐function studies with G protein‐coupled receptors as a paradigm for improving drug discovery and development of therapeutics
Author(s) -
McNeely Patrick M.,
Naranjo Andrea N.,
Robinson Anne S.
Publication year - 2012
Publication title -
biotechnology journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.144
H-Index - 84
eISSN - 1860-7314
pISSN - 1860-6768
DOI - 10.1002/biot.201200076
Subject(s) - g protein coupled receptor , drug discovery , receptor , computational biology , membrane protein , drug , biology , drug development , function (biology) , bioinformatics , microbiology and biotechnology , pharmacology , membrane , biochemistry
There are a great variety of human membrane proteins, and these currently form the largest group of targets for marketed drugs. Despite the advances in drug design, however, promiscuity between drug molecules and targets often leads to undesired signaling effects, which result in unintended side effects. In this review, one family of membrane proteins – the G protein‐coupled receptors (GPCRs) – is used as a model to review experimental techniques that may be used to examine the activity of membrane proteins. As these receptors are highly relevant to healthy human physiology and represent the largest family of drug targets, they represent an excellent model for membrane proteins in general. We also review experimental evidence that suggests there may be multiple ways to target a GPCR – and by extension, membrane proteins – to more effectively target unhealthy phenotypes while reducing the occurrence and severity of side effects.