The selective inhibition of phosphatases by natural toxins: the anhydride domain of tautomycin is not a primary factor in controlling PP1/PP2A selectivity

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• 作者：Liu ; Wen ; Sheppeck II ; James E. ; Colby ; David A. ; Huang ; Hsien-Bin ; Nairn ; Angus C. ; Chamberlin ; A. Richard
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2003
• 出版时间：May 5, 2003
• 年：2003
• 卷：13
• 期：9
• 页码：1597-1600
• 全文大小：191 K

文摘

Analogues of the potent and moderately selective PP1/PP2A inhibitor tautomycin (TM) were prepared with modifications in the C1′–C7′ anhydride moiety. While all retain varying degrees of activity within a 3000-fold range of potencies, they also show remarkable constancy in their IC₅₀ ratios, suggesting that the anhydride moiety is not critical in controlling the selectivity of inhibition.