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Epoxide hydrolase

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https://www.readbyqxmd.com/read/28428366/in-vitro-metabolism-of-oprozomib-an-oral-proteasome-inhibitor-role-of-epoxide-hydrolases-and-cytochrome-p450s
#1
Zhican Wang, Ying Fang, Juli Teague, Hansen Wong, Christophe Morisseau, Bruce D Hammock, Dan A Rock, Zhengping Wang
Oprozomib is an oral proteasome inhibitor currently under investigation in patients with hematologic malignancies or solid tumors. Oprozomib elicits potent pharmacological actions by forming a covalent bond with the active site N-terminal threonine of the 20S proteasome. Oprozomib has a short half-life across preclinical species and in patients due to systemic clearance via metabolism. Potential for drug-drug interactions (DDIs) could alter the exposure of this potent therapeutic therefore a thorough investigation of pathways responsible for metabolism is required...
April 20, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28408149/leptinotarsa-cap-n-collar-isoform-c-kelch-like-ech-associated-protein%C3%A2-1-signaling-is-critical-for-the-regulation-of-ecdysteroidogenesis-in-the-larvae
#2
Qiang-Kun Sun, Qing-Wei Meng, Qing-Yu Xu, Pan Deng, Wen-Chao Guo, Guo-Qing Li
Drosophila cap 'n' collar isoform C (CncC) and Kelch-like ECH associated protein 1 (Keap1) regulate metamorphosis by transcriptional control of a subset of genes involved in ecdysteroidogenesis, 20-hydroxyecdysone (20E) signaling, and juvenile hormone (JH) degradation. In the present paper, we found that prothoracicotropic hormone signal was required for the activation of LdCncC and LdKeap1 in Leptinotarsa decemlineata. Moreover, RNA interference of LdCncC or LdKeap1 in the fourth-instar larvae delayed development...
April 10, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28403941/obesity-is-positively-associated-with-arachidonic-acid-derived-5-and-11-hydroxyeicosatetraenoic-acid-hete
#3
Charles Austin Pickens, Lorraine M Sordillo, Chen Zhang, Jenifer I Fenton
BACKGROUND: Oxylipids are oxygenated polyunsaturated fatty acid (PUFA) metabolites that are responsible for the onset and resolution of the inflammatory response. Enzymatic oxygenation through the lipoxygenase (LOX) or cytochrome P450 (CYP) pathways can form oxylipids that have either proinflammatory or proresolving functions depending on the type of PUFA substrate and degree of metabolism. The objective of this study was to determine how PUFA substrates and their corresponding oxylipids are associated with obesity...
May 2017: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/28400585/juvenile-hormone-epoxide-hydrolase-a-promising-target-for-hemipteran-pest-management
#4
Abudourusuli Tusun, Ming Li, Xiangzhi Liang, Ting Yang, Bin Yang, Guirong Wang
Juvenile hormone epoxide hydrolase (JHEH) has attracted great interest because of its critical role in the regulation of juvenile hormone (JH) in insects. In this study, one JHEH gene from Apolygus lucorum (AlucJHEH) was characterized in terms of deduced amino acid sequence, phylogeny, homology modeling and docking simulation. The results reveals a conserved catalytic mechanism of AlucJHEH toward JH. Our study also demonstrates that the mRNA of AlucJHEH gene was detectable in head, thorax and abdomen from all life stages...
April 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28396419/cyclooxygenase-derived-proangiogenic-metabolites-of-epoxyeicosatrienoic-acids
#5
Amy A Rand, Bogdan Barnych, Christophe Morisseau, Tomas Cajka, Kin Sing Stephen Lee, Dipak Panigrahy, Bruce D Hammock
Arachidonic acid (ARA) is metabolized by cyclooxygenase (COX) and cytochrome P450 to produce proangiogenic metabolites. Specifically, epoxyeicosatrienoic acids (EETs) produced from the P450 pathway are angiogenic, inducing cancer tumor growth. A previous study showed that inhibiting soluble epoxide hydrolase (sEH) increased EET concentration and mildly promoted tumor growth. However, inhibiting both sEH and COX led to a dramatic decrease in tumor growth, suggesting that the contribution of EETs to angiogenesis and subsequent tumor growth may be attributed to downstream metabolites formed by COX...
April 10, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28392259/active-site-flexibility-and-substrate-specificity-in-a-bacterial-virulence-factor-crystallographic-snapshots-of-an-epoxide-hydrolase
#6
Kelli L Hvorecny, Christopher D Bahl, Seiya Kitamura, Kin Sing Stephen Lee, Bruce D Hammock, Christophe Morisseau, Dean R Madden
Pseudomonas aeruginosa secretes an epoxide hydrolase with catalytic activity that triggers degradation of the cystic fibrosis transmembrane conductance regulator (CFTR) and perturbs other host defense networks. Targets of this CFTR inhibitory factor (Cif) are largely unknown, but include an epoxy-fatty acid. In this class of signaling molecules, chirality can be an important determinant of physiological output and potency. Here we explore the active-site chemistry of this two-step α/β-hydrolase and its implications for an emerging class of virulence enzymes...
March 31, 2017: Structure
https://www.readbyqxmd.com/read/28384353/generation-and-characterization-of-epoxide-hydrolase-3-ephx3-deficient-mice
#7
Samantha L Hoopes, Artiom Gruzdev, Matthew L Edin, Joan P Graves, J Alyce Bradbury, Gordon P Flake, Fred B Lih, Laura M DeGraff, Darryl C Zeldin
Cytochrome P450 (CYP) epoxygenases metabolize arachidonic acid into epoxyeicosatrienoic acids (EETs), which play an important role in blood pressure regulation, protection against ischemia-reperfusion injury, angiogenesis, and inflammation. Epoxide hydrolases metabolize EETs to their corresponding diols (dihydroxyeicosatrienoic acids; DHETs) which are biologically less active. Microsomal epoxide hydrolase (EPHX1, mEH) and soluble epoxide hydrolase (EPHX2, sEH) were identified >30 years ago and are capable of hydrolyzing EETs to DHETs...
2017: PloS One
https://www.readbyqxmd.com/read/28378221/bioresolution-of-racemic-phenyl-glycidyl-ether-by-a-putative-recombinant-epoxide-hydrolase-from-streptomyces-griseus-nbrc-13350
#8
Priya Saini, Naveen Kumar, Shadil Ibrahim Wani, Shilpi Sharma, Swapandeep Singh Chimni, Dipti Sareen
In order to produce enantiomerically pure epoxides for the synthesis of value-added chemicals, a novel putative epoxide hydrolase (EH) sgeh was cloned and overexpressed in pET28a/Escherichia coli BL21(DE3). The 1047 bp sgeh gene was mined from Streptomyces griseus NBRC 13350 genome sequence. The recombinant hexahistidyl-tagged SGEH was purified (16.6-fold) by immobilized metal-affinity chromatography, with 90% yield as a homodimer of 100 kDa. The recombinant E. coli whole cells overexpressing SGEH could kinetically resolve racemic phenyl glycidyl ether (PGE) into (R)-PGE with 98% ee, 40% yield, and enantiomeric ratio (E) of 20...
May 2017: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28356494/soluble-epoxide-hydrolase-pharmacological-inhibition-decreases-alveolar-bone-loss-by-modulating-host-inflammatory-response-rank-related-signaling-er-stress-and-apoptosis
#9
Carlos A Trindade da Silva, Ahmed Bettaieb, Marcelo H Napimoga, Kin Sing Stephen Lee, Bora Inceoglu, Carlos Ueira-Vieira, Donald Bruun, Sumanta K Goswami, Fawaz G Haj, Bruce D Hammock
Epoxyeicosatrienoic acids (EETs), metabolites of arachidonic acid derived from the cytochrome P450 (CYP450) enzymes, are mainly metabolized by soluble epoxide hydrolase (sEH) to their corresponding diols. EETs but not their diols, have anti-inflammatory properties and inhibition of sEH might provide protective effects against inflammatory bone loss. Thus, in the present study, we tested the selective sEH inhibitor, 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) in a mouse model of periodontitis induced by infection with A...
March 29, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28332266/11-12-epoxyeicosatrienoic-acid-induces-vasodilator-response-in-the-rat-perfused-mesenteric-vasculature
#10
S M Bihzad, M H M Yousif
Epoxyeicosatrienoic acids (EETs) are endogenous ligands that undergo hydrolysis by soluble epoxide hydrolase (sEH). The responses of 11, 12-EET in comparison with other vasodilator agonists including carbachol and sodium nitroprusside (SNP) were investigated. The effect of 1-cyclohexyl-3-dodecyl urea (CDU), a sEH, was tested on the vasodilator effect induced by 11, 12-EET in the perfused mesenteric beds isolated from normo-glycaemic and type-1 STZ-diabetic rats. In the perfused mesenteric beds of control and diabetic animals, 11, 12-EET produced vasodilation in a dose-dependent manner...
January 2017: Autonomic & Autacoid Pharmacology
https://www.readbyqxmd.com/read/28298080/unraveling-energy-and-dynamics-determinants-to-interpret-protein-functional-plasticity-the-limonene-1-2-epoxide-hydrolases-case-study
#11
Silvia Rinaldi, Alessandro Gori, Celeste Annovazzi, Erica Elisa Ferrandi, Daniela Monti, Giorgio Colombo
The balance between structural stability and functional plasticity in proteins that share common three-dimensional folds is the key factor that drives protein evolvability. The ability to distinguish the parts of homologous proteins that underlie common structural organization patterns from the parts acting as regulatory modules that can sustain modifications in response to evolutionary pressure may provide fundamental insights for understanding sequence-structure-dynamics relationships. In applicative terms, this would help develop rational protein design methods...
March 15, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28296232/inhibitors-of-soluble-epoxide-hydrolase-minimize-ischemia-reperfusion-induced-cardiac-damage-in-normal-hypertensive-and-diabetic-rats
#12
Oliul Islam, Prashanth Patil, Sumanta K Goswami, Rema Razdan, Mohammed N Inamdar, Mohammed Rizwan, Jubin Mathew, Bora Inceoglu, Kin S Stephen Lee, Sung H Hwang, Bruce D Hammock
AIM: We designed a study to evaluate the cardioprotective effect of two soluble epoxide hydrolase (sEH) inhibitors, 1-(1-propanoylpiperidin-4-yl)-3-(4-trifluoromethoxy)phenyl)urea (TPPU) and trans-4-{4-[3-(4-trifluoromethoxyphenyl)-ureido]cyclohexyloxy}benzoic acid (t-TUCB), in ischemia-reperfusion (IR) model. METHODS: Cardioprotective effects of the sEH inhibitors were evaluated against IR-induced myocardial damage in hearts from normal, hypertensive and diabetic rats using Langendorff's apparatus...
March 15, 2017: Cardiovascular Therapeutics
https://www.readbyqxmd.com/read/28295428/atheroprotective-effects-and-molecular-targets-of-tanshinones-derived-from-herbal-medicine-danshen
#13
REVIEW
Jian Fang, Peter J Little, Suowen Xu
Medicinal plant-derived bioactive compounds modulate multiple therapeutic targets in cardiovascular diseases (CVDs), rendering herb-derived phytochemicals effective against one of the major CVDs-atherosclerosis. Danshen (Salvia milthiorriza Bunge) is a Chinese medicine that has been used in cardio- and cerebro-vascular therapeutic remedies in Asian countries for many years. Emerging evidence from cellular, animal, and clinical studies suggests that major lipophilic tanshinones from Danshen can treat atherosclerotic CVDs...
February 16, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/28293507/soluble-epoxide-hydrolase-inhibition-and-epoxyeicosatrienoic-acid-treatment-improve-vascularization-of-engineered-skin-substitutes
#14
Dorothy M Supp, Jennifer M Hahn, Kevin L McFarland, Kelly A Combs, Kin Sing Stephen Lee, Bora Inceoglu, Debin Wan, Steven T Boyce, Bruce D Hammock
BACKGROUND: Autologous engineered skin substitutes comprised of keratinocytes, fibroblasts, and biopolymers can serve as an adjunctive treatment for excised burns. However, engineered skin lacks a vascular plexus at the time of grafting, leading to slower vascularization and reduced rates of engraftment compared with autograft. Hypothetically, vascularization of engineered skin grafts can be improved by treatment with proangiogenic agents at the time of grafting. Epoxyeicosatrienoic acids (EETs) are cytochrome P450 metabolites of arachidonic acid that are inactivated by soluble epoxide hydrolase (sEH)...
December 2016: Plastic and Reconstructive Surgery. Global Open
https://www.readbyqxmd.com/read/28291596/isolation-and-characterization-of-9-lipoxygenase-and-epoxide-hydrolase-2-genes-insight-into-lactone-biosynthesis-in-mango-fruit-mangifera-indica-l
#15
Ashish B Deshpande, Hemangi G Chidley, Pranjali S Oak, Keshav H Pujari, Ashok P Giri, Vidya S Gupta
Uniqueness and diversity of mango flavour across various cultivars are well known. Among various flavour metabolites lactones form an important class of aroma volatiles in certain mango varieties due to their ripening specific appearance and lower odour detection threshold. In spite of their biological and biochemical importance, lactone biosynthetic pathway in plants remains elusive. Present study encompasses quantitative real-time analysis of 9-lipoxygenase (Mi9LOX), epoxide hydrolase 2 (MiEH2), peroxygenase, hydroperoxide lyase and acyl-CoA-oxidase genes during various developmental and ripening stages in fruit of Alphonso, Pairi and Kent cultivars with high, low and no lactone content and explains their variable lactone content...
March 10, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28281333/discovering-drugs-with-dna-encoded-library-technology-from-concept-to-clinic-with-an-inhibitor-of-soluble-epoxide-hydrolase
#16
Svetlana Belyanskaya, Yun Ding, James Callahan, Aili Lazaar, David Israel
DNA encoded chemical library technology was developed with the vision of becoming a transformational platform for drug discovery. The hope was that a new screening paradigm for low molecular weight drugs would be enabled by combining the vast molecular diversity achievable with combinatorial chemistry, the information encoding attributes of DNA, the power of molecular biology and a streamlined selection-based discovery process. We describe the discovery and early clinical development of GSK2256294, an inhibitor of the enzyme soluble epoxide hydrolase (sEH, EPHX2) using Encoded Library Technology (ELT)...
March 9, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28279529/soluble-epoxide-hydrolase-inhibitors-of-indolinone-alkaloids-and-phenolic-derivatives-from-cimicifuga-dahurica-turcz-maxim
#17
Nguyen Phuong Thao, Bui Thi Thuy Luyen, Ji Sun Lee, Jang Hoon Kim, Young Ho Kim
The aim of this study was to search for potential therapeutic agents by identifying novel inhibitors of soluble epoxide hydrolase (sEH) from natural plants using an in silico approach. We found that an ethanolic extract from the roots of Cimicifuga dahurica (Turcz.) Maxim. significantly inhibited sEH in vitro. In a phytochemical investigation using assay-guided fractionation of the dichloromethane extract of C. dahurica, we isolated two new indolinone alkaloids (5 and 6) and five related constituents (1-4, and 7) and established their structures based on an extensive analysis using 1D and 2D NMR, and MS methods...
February 9, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28271340/an-overview-on-the-enhancement-of-enantioselectivity-and-stability-of-microbial-epoxide-hydrolases
#18
REVIEW
Priya Saini, Dipti Sareen
Epoxide hydrolases (EHs; 3.3.2.x) catalyze the enantioselective ring opening of racemic epoxides to the corresponding enantiopure vicinal diols and remaining equivalent unreacted epoxides. These epoxides and diols are used for the synthesis of chiral drug intermediates. With an upsurge in the methods for identification of novel microbial EHs, a lot of EHs have been discovered and utilized for kinetic resolution of racemic epoxides. However, there is still a constraint on the account of limited EHs being successfully applied on the preparative scale for industrial biotransformations...
March 2017: Molecular Biotechnology
https://www.readbyqxmd.com/read/28270581/reply-to-misclassification-of-pfeh1-and-pfeh2-as-epoxide-hydrolases
#19
Daniel E Goldberg, Natalie J Spillman
No abstract text is available yet for this article.
March 7, 2017: MBio
https://www.readbyqxmd.com/read/28259677/soluble-epoxide-hydrolase-inhibition-alleviates-neuropathy-in-akita-ins2-akita-mice
#20
Karen Wagner, Jennifer Gilda, Jun Yang, Debin Wan, Christophe Morisseau, Aldrin V Gomes, Bruce D Hammock
The soluble epoxide hydrolase (sEH) is a regulatory enzyme responsible for the metabolism of bioactive lipid epoxides of both omega-6 and omega-3 long chain polyunsaturated fatty acids. These natural epoxides mediate cell signaling in several physiological functions including blocking inflammation, high blood pressure and both inflammatory and neuropathic pain. Inhibition of the sEH maintains the level of endogenous bioactive epoxy-fatty acids (EpFA) and allows them to exert their generally beneficial effects...
March 1, 2017: Behavioural Brain Research
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