2-(3-Oxo-1, 3-diphenylpropyl) malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: development and prodrug concept

A Wilhelm, LA Lopez-Garcia, K Busschots…

文献索引：Wilhelm, Adriana; Lopez-Garcia, Laura A.; Busschots, Katrien; Froehner, Wolfgang; Maurer, Frauke; Boettcher, Stefan; Zhang, Hua; Schulze, Joerg O.; Biondi, Ricardo M.; Engel, Matthias Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9817 - 9830

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被引用次数: 21

摘要

The protein kinase C-related kinase 2 (PRK2)-interacting fragment (PIF) pocket of phosphoinositide-dependent kinase-1 (PDK1) was proposed as a novel target site for allosteric modulators. In the present work, we describe the design, synthesis, and structure– activity relationship of a series of 2-(3-oxo-1, 3-diphenylpropyl) malonic acids as potent allosteric activators binding to the PIF pocket. Some congeners displayed AC50 values for ...