Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors. |
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Authors: | C E O'Connell K Ackermann C A Rowell A M Garcia M D Lewis C E Schwartz |
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Institution: | Eisai Research Institute, Andover, MA 01810, USA. |
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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). |
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