Synthesis and conformational analysis of peptide inhibitors of farnesyltransferase

…, Y Lelievre, M Duchesne, FF Clerc, D Scherman…

文献索引：Byk, Gerardo; Lelievre, Yves; Duchesne, Marc; Clerc, Francois F.; Scherman, Daniel; Guitton, Jean Dominique Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 1 p. 115 - 124

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被引用次数: 15

摘要

Farnesylation of the ras oncogene product by Farnesyl Transferase (FTase) is known to be a critical step in cell transformation leading to uncontrolled proliferation. The peptide CysValTicMet is a potent FTase inhibitor, but its degradation by amino-peptidases and its only weak internalization into cells make it a bad candidate for a future cancer drug. We have prepared improved CysValTicMet analogues using several approaches:(i) amino ...

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