Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides
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. © 2013 Elsevier Ltd. All rights reserved.
Publication Source (Journal or Book title)
Bioorganic and Medicinal Chemistry Letters
Morisseau, C., Pakhomova, S., Hwang, S., Newcomer, M., & Hammock, B. (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