title: RGS17: an emerging therapeutic target for lung and prostate cancers.
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.
authors.affiliation: The Department of Pharmaceutical Sciences & Experimental Therapeutics, University of Iowa, College of Pharmacy, Iowa City, IA, USA.
authors.forename: Christopher R
authors.initials: CR
authors.lastname: Bodle
authors.forename: Duncan I
authors.initials: DI
authors.lastname: Mackie
authors.forename: David L
authors.initials: DL
authors.lastname: Roman
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D004298:Dopamine / Q000378:metabolism; D019008:Drug Resistance, Neoplasm; D044385:GTP-Binding Protein alpha Subunits / Q000378:metabolism; D020962:Heterotrimeric GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D008024:Ligands; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D020710:RGS Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000378:metabolism; D015398:Signal Transduction
chemical_list: D000970:Antineoplastic Agents; D044385:GTP-Binding Protein alpha Subunits; D008024:Ligands; D020710:RGS Proteins; D017450:Receptors, Opioid, mu; D020962:Heterotrimeric GTP-Binding Proteins; D004298:Dopamine