TY - JOUR
T1 - Evaluating modulators of "regulator of G-protein signaling" (RGS) proteins
AU - Bosch, Dustin E.
AU - Zielinski, Thomas
AU - Lowery, Robert G.
AU - Siderovski, David P.
PY - 2012/3
Y1 - 2012/3
N2 - "Regulator of G-protein Signaling" (RGS) proteins constitute a class of intracellular signaling regulators that accelerate GTP hydrolysis by heterotrimeric Gα subunits. In recent years, RGS proteins have emerged as potential drug targets for modulation by small molecules. Described in this unit are high-throughput screening procedures for identifying modulators of RGS protein-mediated GTPase acceleration (GAP activity), for assessment of RGS domain/Gα interactions (most avid in vitro when Gα is bound by aluminum tetrafluoride), and for validation of candidate GAP-modulatory molecules with the single-turnoverGTP hydrolysis assay.
AB - "Regulator of G-protein Signaling" (RGS) proteins constitute a class of intracellular signaling regulators that accelerate GTP hydrolysis by heterotrimeric Gα subunits. In recent years, RGS proteins have emerged as potential drug targets for modulation by small molecules. Described in this unit are high-throughput screening procedures for identifying modulators of RGS protein-mediated GTPase acceleration (GAP activity), for assessment of RGS domain/Gα interactions (most avid in vitro when Gα is bound by aluminum tetrafluoride), and for validation of candidate GAP-modulatory molecules with the single-turnoverGTP hydrolysis assay.
KW - Fluorescence polarization (FP)
KW - Förster resonance energy transfer (FRET)
KW - Heterotrimeric G-protein α subunits
KW - Regulator of G-protein signaling (RGS) proteins
KW - Single-turnover GTP hydrolysis
UR - http://www.scopus.com/inward/record.url?scp=84860342873&partnerID=8YFLogxK
U2 - 10.1002/0471141755.ph0208s56
DO - 10.1002/0471141755.ph0208s56
M3 - Article
C2 - 22382998
AN - SCOPUS:84860342873
SN - 1934-8282
JO - Current Protocols in Pharmacology
JF - Current Protocols in Pharmacology
IS - SUPPL.56
M1 - 2.8
ER -