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Title: Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.

Authors: Morisseau, Christophe; Pakhomova, Svitlana; Hwang, Sung Hee; Newcomer, Marcia E; Hammock, Bruce D

Published In Bioorg Med Chem Lett, (2013 Jul 01)

Abstract: The soluble epoxide hydrolase (sEH) is a key enzyme in the metabolism of epoxy-fatty acids, signaling molecules involved in numerous biologies. Toward finding novel inhibitors of sEH, a library of known drugs was tested for inhibition of sEH. We found that fulvestrant, an anticancer agent, is a potent (KI=26 nM) competitive inhibitor of sEH. From this observation, we found that alkyl-sulfoxides represent a new kind of pharmacophore for the inhibition of sEH.

PubMed ID: 23684894 Exiting the NIEHS site

MeSH Terms: Dose-Response Relationship, Drug; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology*; Epoxide Hydrolases/antagonists & inhibitors*; Epoxide Hydrolases/metabolism; Estradiol/analogs & derivatives*; Estradiol/chemistry; Estradiol/pharmacology; Humans; Molecular Structure; Solubility; Structure-Activity Relationship; Sulfoxides/chemistry; Sulfoxides/pharmacology*

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