Format

Send to

Choose Destination
See comment in PubMed Commons below
Trends Pharmacol Sci. 2005 Nov;26(11):595-602. Epub 2005 Sep 23.

Techniques: promiscuous Galpha proteins in basic research and drug discovery.

Author information

1
7TM Pharma A/S, 3 Fremtidsvej, 2970 Hoersholm, Denmark. ek@7tm.com

Abstract

Assay technologies that measure the activation of heterotrimeric (alphabetagamma) G proteins by G-protein-coupled receptors (GPCRs) are well established within the pharmaceutical industry, either for pharmacological characterization or for the identification of natural or surrogate receptor ligands. Despite recent evidence indicating that GPCR-linked signalling events might not be mediated exclusively by G proteins, G-protein activation remains a common benchmark for assessing GPCR family members. Thus, assay systems that translate ligand-mediated modulation of GPCRs into G-protein-dependent intracellular responses still represent key components of both basic research and the drug discovery process. In this article, the current knowledge and recent progress of integrating Galpha subunits into assay systems for GPCR drug discovery will be reviewed. Emphasis is given to novel promiscuous and chimeric Galpha proteins. Because of their ability to interact with a wide range of GPCRs, such novel G proteins are likely to be incorporated rapidly into drug discovery programmes.

PMID:
16183138
DOI:
10.1016/j.tips.2005.09.007
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Support Center