Identification of E2F-1/Cyclin A antagonists. |
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| Authors: | S K Sharma T M Ramsey Y N Chen W Chen M S Martin K Clune M Sabio K W Bair |
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| Institution: | Oncology Department, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA. sushil.sharma@pharma.novartis.com |
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| Abstract: | A simple method for the synthesis of a rationally designed (S,S)-Pro-Leu]-spirolactam scaffold is described. This was expanded to a small biased library of compounds mimicking the 'ZRXL' motif in order to identify E2F-1/Cyclin A antagonists. The synthesized compounds were evaluated in an E2F-1/Cyclin A binding assay and moderately active analogues were identified. In addition, the critical roles of Phe, Leu, Lys, and Arg residues of the identified motif were determined. |
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