Synthesis of Non-natural, Frame-Shifted Isoprenoid Diphosphate Analogues

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• 作者：Kayla J. Temple ; Elia N. Wright ; Carol A. Fierke ; Richard A. Gibbs
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：December 2, 2016
• 年：2016
• 卷：18
• 期：23
• 页码：6038-6041
• 全文大小：389K
• ISSN：1523-7052

文摘

A set of synthetic approaches was developed and applied to the synthesis of eight frame-shifted isoprenoid diphosphate analogues. These analogues were designed to increase or decrease the methylene units between the double bonds and/or the pyrophosphate moieties of the isoprenoid structure. Evaluation of mammalian GGTase-I and FTase revealed that small structural changes can result in substantial changes in substrate activity.