Identification of potent inhibitors of the chicken soluble epoxide hydrolase
Identification of potent inhibitors of the chicken soluble epoxide hydrolase
复制标题
DOI：
10.1016/j.bmcl.2014.11.053
复制
发表时间：
2015-01-15
影响因子：
2.7
通讯作者：
Morisseau, Christophe
中科院分区：
文献类型：
--
作者：
Shihadih, Diyala S.;Harris, Todd R.;Morisseau, Christophe
In vertebrates, soluble epoxide hydrolase (sEH) hydrolyzes natural epoxy-fatty acids (EpFAs), which are chemical mediators modulating inflammation, pain, and angiogenesis. Chick embryos are used to study angiogenesis, particularly its role in cardiovascular biology and pathology. To find potent and bio-stable inhibitors of the chicken sEH (chxEH) a library of human sEH inhibitors was screened. Derivatives of 1(adamantan-1-yl)-3-(trans-4-phenoxycyclohexyl) urea were found to be very potent tight binding inhibitors (K-1 < 150 pM) of chxEH while being relatively stable in chicken liver microsomes, suggesting their usefulness to study the role of EpFAs in chickens. (C) 2014 Elsevier Ltd. All rights reserved.
