Identification of potent and selective TACE inhibitors via the S1 pocket
Identification of potent and selective TACE inhibitors via the S1 pocket
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DOI：
10.1016/j.bmcl.2006.10.004
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发表时间：
2007-01-01
影响因子：
2.7
通讯作者：
Zhang, Yuhua
中科院分区：
文献类型：
--
作者：
Condon, Jeffrey S.;Joseph-McCarthy, Diane;Zhang, Yuhua
通过关注哌啶β-砜配体的P1部分，我们鉴定了诱导选择性的基序，并产生了一系列TACE抑制剂，其表现出对分离的TACE酶的优异体外效力和对MMPs 1、2、9、13和14的优异选择性。(c)2006爱思唯尔有限公司版权所有。
By focusing on the P1 portion of the piperidine beta-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14. (c) 2006 Elsevier Ltd. All rights reserved.