Wei Ma

TL;DR: A novel class of heat shock protein 90 (Hsp90) inhibitors was developed from an unbiased screen to identify protein targets for a diverse compound library, and optimized analogues exhibited nanomolar antiproliferative activity across multiple cancer cell lines.

TL;DR: The chemoproteomics-based approach, which also provides broad target selectivity information, was used to drive the identification of a potent and orally active Hsp90 inhibitor, SNX-5422, which is currently in phase 1 clinical studies.

TL;DR: X-ray data show that the scaffold binds competitively at the ATP site on Hsp90, and cellular proliferation and client assays demonstrate that members of the series are able to inhibit HSp90 at nanomolar concentrations.

TL;DR: The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula I as discussed by the authors where Q 1 is CR 1, Q 2 is N, Q 4 and Q 5 are each CR 1, Q 3 is CR 2, X 1 is N or CRc, Y is CR c, X 2 and X 3 are each C(R 5 )(R 6 ), R 7 is O.

TL;DR: In the course of the Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity and it was discovered that it had an effect on tubulin polymerization kinetics and was competitive with colchicine.