| Literature DB >> 16759082 |
Ke Ding1, Yipin Lu, Zaneta Nikolovska-Coleska, Guoping Wang, Su Qiu, Sanjeev Shangary, Wei Gao, Dongguang Qin, Jeanne Stuckey, Krzysztof Krajewski, Peter P Roller, Shaomeng Wang.
Abstract
Potent, specific, non-peptide small-molecule inhibitors of the MDM2-p53 interaction were successfully designed. The most potent inhibitor (MI-63) has a K(i) value of 3 nM binding to MDM2 and greater than 10,000-fold selectivity over Bcl-2/Bcl-xL proteins. MI-63 is highly effective in activation of p53 function and in inhibition of cell growth in cancer cells with wild-type p53 status. MI-63 has excellent specificity over cancer cells with deleted p53 and shows a minimal toxicity to normal cells.Entities:
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Year: 2006 PMID： 16759082 DOI： 10.1021/jm051122a
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446