Showing 1-30 of 89 results for "E0887"
XieMei Tang et al.
Critical reviews in eukaryotic gene expression, 22(3), 179-187 (2012-11-13)
Tuberculosis remains one of the most prevalent and deadly infectious diseases, largely due to the emergence of multidrug-resistant and extensive drug-resistant Mycobacterium tuberculosis, especially the coinfection with HIV. Mycobacterium Ag85 complex (Ag85A, B, and C), with a carboxylesterase consensus sequence...
Tomoko Ishizuka et al.
Drug metabolism and disposition: the biological fate of chemicals, 41(11), 1888-1895 (2013-08-16)
Olmesartan medoxomil (OM) is a prodrug-type angiotensin II type 1 receptor blocker (ARB). We recently identified carboxymethylenebutenolidase homolog (CMBL) as the responsible enzyme for OM bioactivation in humans. In the present study, we compared the bioactivating properties of OM with...
Xingyuan Yang et al.
Molecular endocrinology (Baltimore, Md.), 27(1), 116-126 (2012-12-04)
Adipose triglyceride lipase (ATGL) is the key triacylglycerol hydrolase in adipocytes. The precise mechanisms by which ATGL action is regulated by lipid droplet (LD) coat proteins and responds to hormonal stimulation are incompletely defined. By combining usage of loss- and...
On the homology of the active-site peptides of liver carboxylesterases.
R C Augusteyn et al.
Biochimica et biophysica acta, 171(1), 128-137 (1969-01-07)
Noboru Yamamoto et al.
Cancer chemotherapy and pharmacology, 71(6), 1645-1655 (2013-04-26)
LY2334737 is an oral gemcitabine prodrug. This Phase I study assessed the safety and tolerability of LY2334737 in Japanese patients with solid tumors and evaluated pharmacokinetics (PK), pharmacodynamics, and antitumor activity. Patients with advanced/metastatic solid tumors received escalating doses of...
Keun Na et al.
International journal of cancer, 133(2), 408-415 (2013-01-16)
Although alpha-fetoprotein (AFP) is currently the major serologic biomarker for hepatocellular carcinoma (HCC), it cannot efficiently distinguish this cancer from other forms of liver disease in early diagnosis due to its low sensitivity. The aim of this study is to...
Jay O Knipe et al.
Biopharmaceutics & drug disposition, 29(5), 270-279 (2008-06-13)
The phosphate ester, BMS-292655, was developed as a water-soluble prodrug of the antifungal agent, ravuconazole (BMS-207147). BMS-292655 was comparatively stable in rat, beagle dog, cynomolgus monkey and human plasma, but was hydrolysed upon incubation with liver S9 preparations from all...
Keiichi Uchida et al.
Journal of pediatric surgery, 48(3), 502-509 (2013-03-14)
Human carboxylesterase 2 (CES2) is the key enzyme for metabolic activation of irinotecan (CPT-11). The aim was to evaluate the clinical implications of CES2 RNA expression in neuroblastoma cells. CES2 RNA expression was determined by real-time reverse transcription-polymerase chain reaction...
Takeshi Hashimoto et al.
Biochemical and biophysical research communications, 440(1), 43-49 (2013-09-18)
A previous study has demonstrated that endurance training under hypoxia results in a greater reduction in body fat mass compared to exercise under normoxia. However, the cellular and molecular mechanisms that underlie this hypoxia-mediated reduction in fat mass remain uncertain....
Z Qiao et al.
The Journal of international medical research, 37(4), 1029-1037 (2009-09-19)
Lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) contributes to atherosclerotic plaque instability and subsequent sudden coronary death. Statins are associated with decreased stroke risk and may improve stability of atherosclerotic plaques. The present study investigated the effect of simvastatin on expression of Lp-PLA(2)...
Nicole Mayer et al.
Nature chemical biology, 9(12), 785-787 (2013-10-08)
Adipose triglyceride lipase (ATGL) is rate limiting in the mobilization of fatty acids from cellular triglyceride stores. This central role in lipolysis marks ATGL as an interesting pharmacological target as deregulated fatty acid metabolism is closely linked to dyslipidemic and...
Pierre-Marie Badin et al.
Endocrinology, 154(4), 1444-1453 (2013-03-09)
Elevated expression/activity of adipose triglyceride lipase (ATGL) and/or reduced activity of hormone-sensitive lipase (HSL) in skeletal muscle are causally linked to insulin resistance in vitro. We investigated here the effect of high-fat feeding on skeletal muscle lipolytic proteins, lipotoxicity, and...
Fatty acid ethyl ester synthase inhibition ameliorates ethanol-induced Ca2+-dependent mitochondrial dysfunction and acute pancreatitis.
Huang W, Booth DM, Cane MC, et al.
Gut, 63(8), 1313-1324 (2014)
Takashi Nishiyama et al.
Acta crystallographica. Section D, Biological crystallography, 69(Pt 1), 44-51 (2013-01-01)
Bacterial biofilm formation is an extremely widespread phenomenon involving the secretion of a protective exopolysaccharide matrix which helps the bacteria to attach to surfaces and to overcome a variety of stresses in different environments. This matrix may also include proteins...
Zhe-Yi Hu et al.
Analytical and bioanalytical chemistry, 405(5), 1695-1704 (2012-12-15)
Dabigatran etexilate (DABE) is an oral prodrug that is rapidly converted by esterases to dabigatran (DAB), a direct inhibitor of thrombin. To elucidate the esterase-mediated metabolic pathway of DABE, a high-performance liquid chromatography/mass spectrometry based metabolite identification and semi-quantitative estimation...
Hansjörg Schwertz et al.
Journal of cardiovascular pharmacology, 52(2), 151-160 (2008-08-02)
Animal data strongly support a role for inflammation in myocardial ischemia reperfusion injury. Attempts at cardioprotection by immunomodulation (such as with the specific C5 antibody pexelizumab) in humans have been disappointing. We hypothesized that a broader spectrum antiinflammatory agent might...
Jianqin Zhang et al.
Chemosphere, 93(6), 1207-1215 (2013-08-01)
Carboxylesterases (CarEs) play key roles in metabolism of specific hormones and detoxification of dietary and environmental xenobiotics in insects. We sequenced and characterized CarE cDNAs putatively derived from two different genes named LmCesA1 and LmCesA2 from the migratory locust, Locusta...
Huili Zhu et al.
Nan fang yi ke da xue xue bao = Journal of Southern Medical University, 33(10), 1499-1503 (2013-10-23)
To investigate the effect of glucagon-like peptide-1 (GLP-1) on glycolipid metabolism in 3T3-L1 adipocytes and explore the mechanism. 3T3-L1 adipocytes were treated with GLP-1, insulin, or both for 24 h, and Western blotting was used to analyze the expression levels...
Anna Sobeková et al.
Acta biologica Hungarica, 60(1), 45-54 (2009-04-22)
The activities of the antioxidant and detoxifying enzymes, superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSHPx), glutathione reductase (GR), glutathione-S-transferase (GST), and the content of thiobarbituric acid reactive substances (TBARS) were determined in the liver and kidney of rabbits after...
Pei-Chi Lee et al.
Biomaterials, 34(34), 8756-8765 (2013-08-14)
In this study, single-walled carbon nanotubes (SWNTs) conjugated with antibody C225 were used to achieve targeted therapy against EGFR over-expressed colorectal cancer cells. In addition, the control release of the chemotherapeutic drug, 7-Ethyl-10-hydroxy-camptothecin (SN38), was studied. We used three different...
Kun Zhang et al.
Archives of insect biochemistry and physiology, 82(4), 213-226 (2013-02-14)
The citrus red mite, Panonychus citri, is known for its ability to rapidly evolve resistance to insecticides/acaricides and to adapt to hosts that produce toxins. To get better insight into the detoxification mechanism of P. citri, two carboxylesterase (CarE) genes...
Rami Akkad et al.
Journal of AOAC International, 95(5), 1371-1377 (2012-11-28)
HPTLC-enzyme inhibition assay was applied to different fruit and vegetable samples after individual spiking with organophosphate and carbamate pesticides at their maximum residue limits documented by the European Commission. Samples were extracted according to the QuEChERS (Quick, Easy, Cheap, Effective...
Shiqi Luo et al.
Gene, 524(2), 275-281 (2013-04-23)
Carboxylesterase (EC 3.1.1.1) is a member of the carboxyl/cholinesterase (CCE) superfamily, which is widely distributed in animals, plants and microorganisms. This enzyme has been known to be associated with insecticide resistance and detoxification. Although CCEs have been extensively studied in...
Panitta Sitthinamsuwan et al.
Journal of the Medical Association of Thailand = Chotmaihet thangphaet, 96(1), 83-90 (2013-06-01)
Neuroendocrine carcinoma (NEC) is a rare entity of uterine cervical carcinoma. Most of them have a more aggressive course and worse prognosis than a common type squamous cell carcinoma. Therefore, precise diagnosis is very crucial. To study clinicopathological correlation and...
Marianne Z Metz et al.
Stem cells translational medicine, 2(12), 983-992 (2013-10-30)
CPT-11 (irinotecan) has been investigated as a treatment for malignant brain tumors. However, limitations of CPT-11 therapy include low levels of the drug entering brain tumor sites and systemic toxicities associated with higher doses. Neural stem cells (NSCs) offer a...
Carboxylesterases (EC 3.1.1). A large-scale purification of pig liver carboxylesterase.
D J Horgan et al.
Biochemistry, 8(5), 2000-2006 (1969-05-01)
J Ozols
The Journal of biological chemistry, 262(31), 15316-15321 (1987-11-05)
A glycoprotein having a subunit weight of approximately 60,000 was isolated from rabbit liver microsomes. It is a predominant component of the hepatic microsomal membrane and reacts rapidly with diisopropylphosphorofluoridate (DFP), resulting in the loss of enzymatic activity toward artificial...
Astrid Schrammel et al.
Biochimica et biophysica acta, 1831(11), 1600-1608 (2013-07-23)
Cardiac oxidative stress has been implicated in the pathogenesis of hypertrophy, cardiomyopathy and heart failure. Systemic deletion of the gene encoding adipose triglyceride lipase (ATGL), the enzyme that catalyzes the rate-limiting step of triglyceride lipolysis, results in a phenotype characterized...
Ian Cushman et al.
The Journal of biological chemistry, 288(26), 19177-19183 (2013-05-10)
A number of proteins that play key roles in cell signaling are post-translationally modified by the prenylation pathway. The final step in this pathway is methylation of the carboxyl terminus of the prenylated protein by isoprenylcysteine carboxylmethyltransferase. Due to the...
Helge Ræder et al.
Diabetes, 63(1), 259-269 (2013-09-26)
Carboxyl-ester lipase (CEL) maturity-onset diabetes of the young (MODY) is a monogenic form of diabetes and pancreatic exocrine dysfunction due to mutations in the CEL gene encoding CEL. The pathogenic mechanism for diabetes development is unknown. Since CEL is expressed...

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