Lipid and sulfur substituted prenylcysteine analogs as human Icmt inhibitors
Lipid and sulfur substituted prenylcysteine analogs as human Icmt inhibitors
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DOI：
10.1016/j.bmcl.2011.06.053
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发表时间：
2011-09-15
影响因子：
2.7
通讯作者：
Gibbs, Richard A.
中科院分区：
文献类型：
--
作者：
Bergman, Joel A.;Hahne, Kalub;Gibbs, Richard A.
Inhibition of isoprenylcysteine carboxyl methyltransferase (Icmt) offers a promising strategy for K-Ras driven cancers. We describe the synthesis and inhibitory activity of substrate-based analogs derived from several novel scaffolds. Modifications of both the prenyl group and thioether of N-acetyl-S-farnesyl-L-cysteine (AFC), a substrate for human Icmt (hIcmt), have resulted in low micromolar inhibitors of Icmt and have given insights into the nature of the prenyl binding site of hIcmt. (C) 2011 Elsevier Ltd. All rights reserved.
