Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I

…, J Ohkanda, SM Sebti, AD Hamilton

文献索引：Qian, Yimin; Vogt, Andreas; Sebti, Said M.; Hamilton, Andrew D. Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 217 - 223

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被引用次数: 89

摘要

The design, synthesis, and biological evaluation of a family of peptidomimetic inhibitors of protein geranylgeranyltransferase-I (PGGTase-I) are reported. The inhibitors are based on the C-terminal CAAL sequence of many geranylgeranylated proteins. Using 2-aryl-4- aminobenzoic acid derivatives as mimetics for the central dipeptide (AA), we have attached a series of imidazole and pyridine derivatives to the N-terminus as cysteine replacements. ...