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RGS17: an emerging therapeutic target for lung and prostate cancers
Journal article   Peer reviewed

RGS17: an emerging therapeutic target for lung and prostate cancers

Christopher R Bodle, Duncan I Mackie and David L Roman
Future medicinal chemistry, Vol.5(9), pp.995-1007
06/2013
DOI: 10.4155/fmc.13.91
PMCID: PMC3865709
PMID: 23734683
url
https://www.ncbi.nlm.nih.gov/pmc/articles/3865709View
Open Access

Abstract

Ligands for G-protein-coupled receptors (GPCRs) represent approximately 50% of currently marketed drugs. RGS proteins modulate heterotrimeric G proteins and, thus, GPCR signaling, by accelerating the intrinsic GTPase activity of the Gα subunit. Given the prevalence of GPCR targeted therapeutics and the role RGS proteins play in G protein signaling, some RGS proteins are emerging as targets in their own right. One such RGS protein is RGS17. Increased RGS17 expression in some prostate and lung cancers has been demonstrated to support cancer progression, while reduced expression of RGS17 can lead to development of chemotherapeutic resistance in ovarian cancer. High-throughput screening is a powerful tool for lead compound identification, and utilization of high-throughput technologies has led to the discovery of several RGS inhibitors, thus far. As screening technologies advance, the identification of novel lead compounds the subsequent development of targeted therapeutics appears promising.

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