Reversible, allosteric small-molecule inhibitors of regulator of g protein signaling proteins.
AuthorsBlazer LL, Roman DL, Chung A, Larsen MJ, Greedy BM, Husbands SM, Neubig RR,
JournalMol Pharmacol
PubMed ID20571077
Regulators of G protein signaling (RGS) proteins are potent negative modulators of G protein signaling and have been proposed as potential targets for small-molecule inhibitor development. We report a high-throughput time-resolved fluorescence resonance energy transfer screen to identify inhibitors of RGS4 and describe the first reversible small-molecule inhibitors of an ... More