PMID- 23684894
OWN - NLM
STAT- MEDLINE
DCOM- 20140113
LR  - 20211021
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Print)
IS  - 0960-894X (Linking)
VI  - 23
IP  - 13
DP  - 2013 Jul 1
TI  - Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.
PG  - 3818-21
LID - S0960-894X(13)00573-8 [pii]
LID - 10.1016/j.bmcl.2013.04.083 [doi]
AB  - 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.
CI  - Copyright (c) 2013 Elsevier Ltd. All rights reserved.
FAU - Morisseau, Christophe
AU  - Morisseau C
AD  - Department of Entomology and UCD Comprehensive Cancer Center, University of 
      California, One Shields Avenue, Davis, CA 95616, USA. chmorisseau@ucdavis.edu
FAU - Pakhomova, Svitlana
AU  - Pakhomova S
FAU - Hwang, Sung Hee
AU  - Hwang SH
FAU - Newcomer, Marcia E
AU  - Newcomer ME
FAU - Hammock, Bruce D
AU  - Hammock BD
LA  - eng
GR  - ES02710/ES/NIEHS NIH HHS/United States
GR  - R01 HL107887/HL/NHLBI NIH HHS/United States
GR  - R01 ES002710/ES/NIEHS NIH HHS/United States
GR  - P42 ES004699/ES/NIEHS NIH HHS/United States
GR  - R01 HL 107887/HL/NHLBI NIH HHS/United States
GR  - P42 ES04699/ES/NIEHS NIH HHS/United States
GR  - R37 ES002710/ES/NIEHS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20130506
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Sulfoxides)
RN  - 22X328QOC4 (Fulvestrant)
RN  - 4TI98Z838E (Estradiol)
RN  - EC 3.3.2.- (Epoxide Hydrolases)
SB  - IM
MH  - Dose-Response Relationship, Drug
MH  - Enzyme Inhibitors/chemistry/*pharmacology
MH  - Epoxide Hydrolases/*antagonists & inhibitors/metabolism
MH  - Estradiol/*analogs & derivatives/chemistry/pharmacology
MH  - Fulvestrant
MH  - Humans
MH  - Molecular Structure
MH  - Solubility
MH  - Structure-Activity Relationship
MH  - Sulfoxides/chemistry/*pharmacology
PMC - PMC3703951
MID - NIHMS476701
EDAT- 2013/05/21 06:00
MHDA- 2014/01/15 06:00
PMCR- 2014/07/01
CRDT- 2013/05/21 06:00
PHST- 2013/04/01 00:00 [received]
PHST- 2013/04/29 00:00 [accepted]
PHST- 2013/05/21 06:00 [entrez]
PHST- 2013/05/21 06:00 [pubmed]
PHST- 2014/01/15 06:00 [medline]
PHST- 2014/07/01 00:00 [pmc-release]
AID - S0960-894X(13)00573-8 [pii]
AID - 10.1016/j.bmcl.2013.04.083 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2013 Jul 1;23(13):3818-21. doi: 10.1016/j.bmcl.2013.04.083. 
      Epub 2013 May 6.