Genetic variations and polymorphisms of G protein-coupled receptors: functional and therapeutic implications.

Abstract:

:G protein-coupled receptors (GPCRs) represent a major class of proteins in the genome of many species, including humans. In addition to the mapping of a number of human disorders to regions of the genome containing GPCRs, a growing body of literature has documented frequently occurring variations (i.e. polymorphisms) in GPCR loci. In this article, we use a domain-based approach to systematically examine examples of genetic variation in the coding and noncoding regions of GPCR loci. Data to date indicate that residues in GPCRs are involved in ligand binding and coupling to G proteins and that regulation can be altered by polymorphisms. Studies of GPCR polymorphisms have also uncovered the functional importance of residues not previously implicated from other approaches that are involved in the function of GPCRs. We predict that studies of GPCR polymorphisms will have a significant impact on medicine and pharmacology, in particular, by providing new means to subclassify patients in terms of both diagnosis and treatment.

authors

Rana BK,Shiina T,Insel PA

doi

10.1146/annurev.pharmtox.41.1.593

keywords:

subject

Has Abstract

pub_date

2001-01-01 00:00:00

pages

593-624

eissn

0362-1642

issn

1545-4304

pii

41/1/593

journal_volume

41

pub_type

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