Examination of phosphoryl-mimicking functionalities within a macrocyclic Grb2 SH2 domain-binding platform

…, PG Dharmawardana, SJ Choyke…

Index: Kang, Sang-Uk; Shi, Zhen-Dan; Worthy, Karen M.; Bindu, Lakshman K.; Dharmawardana, Pathirage G.; Choyke, Sarah J.; Bottaro, Donald P.; Fisher, Robert J.; Burke Jr., Terrence R. Journal of Medicinal Chemistry, 2005 , vol. 48, # 12 p. 3945 - 3948

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Citation Number: 23

Abstract

Reported herein are the design, synthesis, and Grb2 SH2 domain-binding affinities of several phosphoryl-mimicking groups displayed within the context of a conformationally constrained macrocyclic platform. With use of surface plasmon resonance techniques, single- digit nanomolar affinities were exhibited by phosphonic acid and malonyl-containing diacidic phosphoryl mimetics (for 4h and 4g, KD= 1.47 and 3.62 nM, respectively). ...

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