Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides |
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| Authors: | Christophe Morisseau Svitlana Pakhomova Sung Hee Hwang Marcia E Newcomer Bruce D Hammock |
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| Institution: | 1. Department of Entomology and UCD Comprehensive Cancer Center, University of California, One Shields Avenue, Davis, CA 95616, USA;2. Department of Biological Sciences, Louisiana State University, Baton Rouge, LA 70803, USA |
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| 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. |
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| Keywords: | Soluble epoxide hydrolase Epoxy-eicosatrienoic acids Fulvestrant Competitive inhibition X-ray structure |
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