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ID: ALA1132533
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors.
Authors: O'Connell CE, Ackermann K, Rowell CA, Garcia AM, Lewis MD, Schwartz CE.
Abstract: A series of peptidomimetics based on a hydroxyproline scaffold was prepared and evaluated for inhibition of farnesyltransferase and geranylgeranyltransferase I in both enzymatic and cell-based assays. A number of analogs were potent and selective inhibitors of FTase, while one compound (22) was nonselective in the enzymatic assays but eight-fold selective for inhibition of GGTase in the cellular assay (IC50 = 0.39 microM).
CiteXplore: 10450988