Probing the isoprenylcysteine carboxyl methyltransferase (Icmt) binding pocket: Sulfonamide modified farnesyl cysteine (SMFC) analogs as Icmt inhibitors

JD Majmudar, K Hahne, CA Hrycyna…

文献索引：Majmudar, Jaimeen D.; Hahne, Kalub; Hrycyna, Christine A.; Gibbs, Richard A. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 9 p. 2616 - 2620

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被引用次数: 7

摘要

Human isoprenylcysteine carboxyl methyltransferase (hIcmt) is a promising anticancer target as it is important for the post-translational modification of oncogenic Ras proteins. We herein report the synthesis and biochemical activity of 41 farnesyl-cysteine based analogs versus hIcmt. We have demonstrated that the amide linkage of a hIcmt substrate can be replaced by a sulfonamide bond to achieve hIcmt inhibition. The most potent sulfonamide-modified ...