Synthesis and evaluation of some hydroxyproline-derived peptidomimetics as isoprenyltransferase inhibitors.
نویسندگان
چکیده
CA1A2X peptidomimetics containing a modified proline at position A2 were prepared and evaluated for their ability to inhibit farnesyltransferase (FTase) and geranylgeranyltransferase I (GGTase I) in enzymatic and cell-based assays. These compounds inhibited farnesylation of H-ras in vitro in the high nanomolar to low micromolar IC50 range.
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ورودعنوان ژورنال:
- Chemical & pharmaceutical bulletin
دوره 48 5 شماره
صفحات -
تاریخ انتشار 2000