Morisseau_2013_Bioorg.Med.Chem.Lett_23_3818

Reference

Title : Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides - Morisseau_2013_Bioorg.Med.Chem.Lett_23_3818
Author(s) : Morisseau C , Pakhomova S , Hwang SH , Newcomer ME , Hammock BD
Ref : Bioorganic & Medicinal Chemistry Lett , 23 :3818 , 2013
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.

PubMedSearch : Morisseau_2013_Bioorg.Med.Chem.Lett_23_3818
PubMedID: 23684894
Gene_locus related to this paper: human-EPHX2

Related information

Inhibitor Fulvestrant
Gene_locus human-EPHX2
Structure 4J03

Citations formats

Morisseau C, Pakhomova S, Hwang SH, Newcomer ME, Hammock BD (2013)
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides
Bioorganic & Medicinal Chemistry Lett 23 :3818

Morisseau C, Pakhomova S, Hwang SH, Newcomer ME, Hammock BD (2013)
Bioorganic & Medicinal Chemistry Lett 23 :3818