Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides

Christophe Morisseau, Svitlana Pakhomova, Sung Hee Hwang, Marcia E. Newcomer, Bruce D. Hammock

Research output: Contribution to journalArticle

9 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)3818-3821
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number13
DOIs
StatePublished - Jul 1 2013

Keywords

  • Competitive inhibition
  • Epoxy-eicosatrienoic acids
  • Fulvestrant
  • Soluble epoxide hydrolase
  • X-ray structure

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Fingerprint Dive into the research topics of 'Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides'. Together they form a unique fingerprint.

  • Cite this

    Morisseau, C., Pakhomova, S., Hwang, S. H., Newcomer, M. E., & Hammock, B. D. (2013). Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides. Bioorganic and Medicinal Chemistry Letters, 23(13), 3818-3821. https://doi.org/10.1016/j.bmcl.2013.04.083