نتایج جستجو برای: epoxide hydrolase

تعداد نتایج: 26425  

Journal: :Biochemical pharmacology 1982
L S Hasegawa B D Hammock

A continuous spectrophotometric assay based on the differences in the ultraviolet spectra of trans-stilbene oxide (TSO) and its reaction product 1,2-diphenyl-1,2-ethanediol is described for the measurement of mammalian cytosolic epoxide hydrolase activity. Rates of TSO hydration determined by this method were similar to those obtained by independent analytical methods, and the assay is rapid, r...

Journal: :Applied and environmental microbiology 1997
L Bezalel Y Hadar C E Cerniglia

The enzymatic mechanisms involved in the degradation of phenanthrene by the white rot fungus Pleurotus ostreatus were examined. Phase I metabolism (cytochrome P-450 monooxygenase and epoxide hydrolase) and phase II conjugation (glutathione S-transferase, aryl sulfotransferase, UDP-glucuronosyltransferase, and UDP-glucosyltransferase) enzyme activities were determined for mycelial extracts of P....

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2016
Xue-Qing Li Martin A Hayes Gunnar Grönberg Kristina Berggren Neal Castagnoli Lars Weidolf

Oxetane moieties are increasingly being used by the pharmaceutical industry as building blocks in drug candidates because of their pronounced ability to improve physicochemical parameters and metabolic stability of drug candidates. The enzymes that catalyze the biotransformation of the oxetane moiety are, however, not well studied. The in vitro metabolism of a spiro oxetane-containing compound ...

Journal: :Current opinion in pharmacology 2012
Sandrine Silvente-Poirot Marc Poirot

Cholesterol epoxide hydrolase (ChEH) catalyzes the hydration of cholesterol-5,6-epoxides (5,6-EC) into cholestane-3β,5α,6β-triol. ChEH is a hetero-oligomeric complex called the anti-estrogen binding site (AEBS) comprising 3β-hydroxysterol-Δ(8)-Δ(7)-isomerase (D8D7I) and 3β-hydroxysterol-Δ(7)-reductase (DHCR7). D8D7I and DHCR7 regulate cholesterol biosynthesis, fetal development and growth, tumo...

2010
Yi-Xin Jim Wang Arzu Ulu Le-Ning Zhang Bruce Hammock

Like many eicosanoids, epoxyeicosatrienoic acids (EETs) have multiple biological functions, including reduction of blood pressure, inflammation, and atherosclerosis in multiple species. Hydration of EETs by the soluble epoxide hydrolase (sEH) is the major route of their degradation to the less bioactive diols. Inhibition of the sEH stabilizes EETs, thus, enhancing the beneficial effects of EETs...

Journal: :Bioorganic & medicinal chemistry letters 2014
Vladimir Burmistrov Christophe Morisseau Kin Sing Stephen Lee Diyala S Shihadih Todd R Harris Gennady M Butov Bruce D Hammock

A series of inhibitors of the soluble epoxide hydrolase (sEH) containing two urea groups has been developed. Inhibition potency of the described compounds ranges from 2.0 μM to 0.4 nM. 1,6-(Hexamethylene)bis[(adamant-1-yl)urea] (3b) was found to be a potent slow tight binding inhibitor (IC50=0.5 nM) with a strong binding to sEH (Ki=3.1 nM) and a moderately long residence time on the enzyme (kof...

Journal: :Bioorganic & medicinal chemistry letters 2006
Christophe Morisseau John W Newman Hsing-Ju Tsai Preston A Baecker Bruce D Hammock

We prepared a series of amino acid derived cyclohexyl and adamantyl ureas and tested them as inhibitors of the human soluble epoxide hydrolase, and obtained very potent compounds (K(I)=15nM) that are >10-fold more soluble than previously described sEH inhibitors. While our lead compound 2 showed low apparent bioavailability in dogs and rats, this series of compounds revealed that sEH inhibitor ...

Journal: :Journal of medicinal chemistry 2011
In-Hae Kim Yong-Kyu Park Bruce D Hammock Kosuke Nishi

Structure-activity relationships of cycloalkylamide compounds as inhibitors of human sEH were investigated. When the left side of amide function was modified by a variety of cycloalkanes, at least a C6 like cyclohexane was necessary to yield reasonable inhibition potency on the target enzyme. In compounds with a smaller cycloalkane or with a polar group on the left side of amide function, no in...

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