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Identification of potent inhibitors of the chicken soluble epoxide hydrolase.


ABSTRACT: 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 (KI <150pM) of chxEH while being relatively stable in chicken liver microsomes, suggesting their usefulness to study the role of EpFAs in chickens.

SUBMITTER: Shihadih DS 

PROVIDER: S-EPMC4277729 | biostudies-literature | 2015 Jan

REPOSITORIES: biostudies-literature

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Identification of potent inhibitors of the chicken soluble epoxide hydrolase.

Shihadih Diyala S DS   Harris Todd R TR   Yang Jun J   Merzlikin Oleg O   Lee Kin Sing S KS   Hammock Bruce D BD   Morisseau Christophe C  

Bioorganic & medicinal chemistry letters 20141126 2


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  ...[more]

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