利用酶亚位点的原核生物UDP-吡喃半乳糖变位酶的强效配体。
Potent ligands for prokaryotic UDP-galactopyranose mutase that exploit an enzyme subsite.
作者信息
Dykhuizen Emily C, Kiessling Laura L
机构信息
Department of Chemistry, University of Wisconsin-Madison, Madison, Wisconsin 53706, USA.
出版信息
Org Lett. 2009 Jan 1;11(1):193-6. doi: 10.1021/ol802094p.
Abstract
UDP-galactopyranose mutase (UGM or Glf), which catalyzes the interconversion of UDP-galactopyranose and UDP-galactofuranose, is implicated in the viability and virulence of multiple pathogenic microorganisms. Here we report the synthesis of high-affinity ligands for UGM homologues from Klebsiella pneumoniae and Mycobacterium tuberculosis. The potency of these compounds stems from their ability to access both the substrate binding pocket and an adjacent site.
摘要
UDP-吡喃半乳糖变位酶（UGM或Glf）催化UDP-吡喃半乳糖和UDP-呋喃半乳糖的相互转化，与多种致病微生物的生存能力和毒力有关。在此，我们报告了肺炎克雷伯菌和结核分枝杆菌UGM同源物的高亲和力配体的合成。这些化合物的效力源于它们能够同时进入底物结合口袋和相邻位点。
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