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Assay Method Information

Assay Name:  Dose response, multiplexed high-throughput screen for small molecule regulators of RGS family protein interactions, specifically RGS8-Galphao for SAR Compounds
Description:  University of New Mexico Assay Overview: Assay Support: NIH R21NS057014 HTS to identify small molecule regulators of RGS family protein interactions PI: Richard Neubig, Ph.D. Assay Implementation: Yang Wu Ph.D., Mark Haynes Ph.D., Anna Waller Ph.D., Mark Carter MS Target Team Leader for the Center: Larry Sklar, Ph.D., (lsklar@salud.unm.edu) Assay Background and Significance: Regulators of G protein signaling (RGS) proteins are a diverse set of intracellular proteins that modulate G protein-coupled receptor (GPCR) signaling [Neitzel and Hepler, 2006]. Their diversity is a result of their localized tissue distribution as well as their preferential regulation of a particular subunit of G protein (Galpha) [Zhong and Neubig, 2001; Neubig and Siderovski, 2002]. Following activation by ligand-bound GPCRs, the Galpha subunit undergoes rapid GTP - GDP exchange, and subsequently dissociates from both the GPCR and the G protein beta-gamma subunit (Gbg). Active GTP-bound Galpha (Galpha-GTP)
Affinity data for this assay
 

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Last update November 1, 2007
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