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
Full Text: HTML
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). ...
Related Articles:
[Soi, Antonio; Pfeiffer, Jens; Jauch, Johann; Schurig, Volker Tetrahedron Asymmetry, 1999 , vol. 10, # 1 p. 177 - 182]
A Simple Regioselective Nuclear Bromination of Alkyl Phenyl Ethers
[Yakabe, Shigetaka; Hirano, Masao; Morimoto, Takashi Organic Preparations and Procedures International, 1998 , vol. 30, # 2 p. 218 - 222]
[Rogers, Harold R.; Houk, Janette Journal of the American Chemical Society, 1982 , vol. 104, # 2 p. 522 - 525]
An Eco-Sustainable Erbium (III) Triflate Catalyzed Formation and Cleavage of tert-Butyl Ethers
[Procopio, Antonio; Costanzo, Paola; Curini, Massimo; Nardi, Monica; Oliverio, Manuela; Paonessa, Rosina Synthesis, 2011 , # 1 p. 73 - 78]