The discovery of novel tartrate-based TNF-α converting enzyme (TACE) inhibitors
A novel series of TNF-α convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of l-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner. They are selective for TACE over other MMP's. We report the first X-ray crystal structure for a tartrate-based TACE inhibitor.
Rosner, Kristin E.,Guo, Zhuyan,Orth, Peter,Shipps Jr., Gerald W.,Belanger, David B.,Chan, Tin Yau,Curran, Patrick J.,Dai, Chaoyang,Deng, Yongqi,Girijavallabhan, Vinay M.,Hong, Liwu,Lavey, Brian J.,Lee, Joe F.,Li, Dansu,Liu, Zhidan,Popovici-Muller, Janeta,Ting, Pauline C.,Vaccaro, Henry,Wang, Li,Wang, Tong,Yu, Wensheng,Zhou, Guowei,Niu, Xiaoda,Sun, Jing,Kozlowski, Joseph A.,Lundell, Daniel J.,Madison, Vincent,McKittrick, Brian,Piwinski, John J.,Shih, Neng -Yang,Arshad Siddiqui,Strickland, Corey O.
scheme or table
p. 1189 - 1193
(2010/05/19)
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