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 |
Inhibitor | Fulvestrant |
Gene_locus | human-EPHX2 |
Structure | 4J03 |
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