Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides: part II

通过使用 N-取代哌啶基二苯磺酰基磺酰胺抑制分泌型卷曲相关蛋白 I (sFRP-1) 来调节 Wnt 信号传导:第二部分

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作者:William J Moore, Jeffrey C Kern, Ramesh Bhat, Peter V N Bodine, Shoichi Fukyama, Girija Krishnamurthy, Ronald L Magolda, Keith Pitts, Barb Stauffer, Eugene J Trybulski

Abstract

Piperidinyl diphenylsulfonyl sulfonamides are a novel class of molecules that have inhibitory binding affinity for sFRP-1. As a secreted protein sFRP-1 inhibits the function of the secreted Wnt glycoprotein. Therefore, as inhibitors of sFRP-1 these small molecules facilitate the Wnt/beta-catenin canonical signaling pathway. Details of the structure-activity relationships and biological activity of this structural class of compounds will be discussed.

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