Hsp90 maintains the conformational stability of multiple proteins implicated in oncogenesis and has emerged as a target for chemotherapy. We report here the discovery of a novel small molecule scaffold that inhibits Hsp90. X-ray data show that the scaffold binds competitively at the ATP site on Hsp90. Cellular proliferation and client assays demonstrate that members of the series are able to inhibit Hsp90 at nanomolar concentrations.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2008.05.023 | DOI Listing |
Publication Analysis
Top Keywords
novel small
8
small molecule
8
hsp90
5
discovery benzamide
4
benzamide tetrahydro-4h-carbazol-4-ones
4
tetrahydro-4h-carbazol-4-ones novel
4
molecule inhibitors
4
inhibitors hsp90
4
hsp90 hsp90
4
hsp90 maintains
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!