Title : High-throughput screening for small-molecule inhibitors of LARG-stimulated RhoA nucleotide binding via a novel fluorescence polarization assay.

Pub. Date : 2009 Feb

PMID : 19196702






2 Functional Relationships(s)
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1 Using a novel fluorescence polarization guanine nucleotide-binding assay using BODIPY-Texas Red-GTPgammaS (BODIPY-TR-GTPgammaS), the authors performed a 10,000-compound high-throughput screen for inhibitors of LARG-stimulated RhoA nucleotide binding. Guanine Nucleotides Rho guanine nucleotide exchange factor 12 Homo sapiens
2 Five compounds identified from the high-throughput screen were confirmed in a nonfluorescent radioactive guanine nucleotide-binding assay measuring LARG-stimulated [( 35)S] GTPgammaS binding to RhoA, thus ruling out nonspecific fluorescent effects. Guanine Nucleotides Rho guanine nucleotide exchange factor 12 Homo sapiens