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pubmed:abstractText |
The rational design of peptide-based specific inhibitors of the caspase family members using their X-ray crystallographies is an important strategy for chemical knockdown to define the critical role of each enzyme in apoptosis and inflammation. Recently, we designed a novel potent peptide inhibitor, Ac-DNLD-CHO, for caspase-3 using a new computational screening system named the Amino acid Positional Fitness (APF) method (BMC Pharmacol. 2004, 4:7). Here, we report the specificity of the DNLD sequence against caspase-3 over other major caspase family members that participate in apoptosis by computational docking and site-directed mutagenesis studies.
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pubmed:affiliation |
Department of Biochemistry, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Yamazaki Noda, Chiba, Japan. yosimori@rs.noda.tus.ac.jp <yosimori@rs.noda.tus.ac.jp>
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