| Literature DB >> 15664854 |
Daniel J Parks1, Louis V Lafrance, Raul R Calvo, Karen L Milkiewicz, Varsha Gupta, Jennifer Lattanze, Kannan Ramachandren, Theodore E Carver, Eugene C Petrella, Maxwell D Cummings, Diane Maguire, Bruce L Grasberger, Tianbao Lu.
Abstract
A library of 1,4-benzodiazepine-2,5-diones was screened for binding to the p53-binding domain of HDM2 using Thermofluor, a miniaturized thermal denaturation assay. The hits obtained were shown to bind to HDM2 in the p53-binding pocket using a fluorescence polarization (FP) peptide displacement assay. The potency of the series was optimized, leading to sub-micromolar antagonists of the p53-HDM2 interaction.Entities:
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Year: 2005 PMID： 15664854 DOI： 10.1016/j.bmcl.2004.11.009
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823