Barta Thomas E

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 present results demonstrate that a small molecule Hsp90 inhibitor can impact inflammatory disease processes and provides preclinical validation for consideration of Hsp 90 inhibitors in the treatment of RA.

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: α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP's-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system.