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Keyword:'A9272'
Showing 1-30 of 32 results for "A9272" within Papers
Sumit Bansal et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 1011, 171-178 (2016-01-17)
Detoxification of lithocholic acid (LCA) to lithocholic acid sulfate (LCA-S) is catalyzed by sulfotransferases, mainly SULT2A1. We developed and validated an ultra-high performance liquid chromatography-tandem mass spectrometric (UPLC-MS/MS) method to quantify human liver cytosolic-dependent LCA sulfation. Chromatographic separation was achieved
Jessica Perrin et al.
Nature biotechnology, 38(3), 303-308 (2020-01-22)
Monitoring drug-target interactions with methods such as the cellular thermal-shift assay (CETSA) is well established for simple cell systems but remains challenging in vivo. Here we introduce tissue thermal proteome profiling (tissue-TPP), which measures binding of small-molecule drugs to proteins
Nattha Yongwattana et al.
Molecules (Basel, Switzerland), 25(5) (2020-03-07)
Calcium pyrophosphate deposition disease (CPPD) is a crystal induced inflammation in joints, and causes severe pain in elderly people. The accumulation of pyrophosphate (PPi) in synovial fluid (SF) results from several enzymatic reactions, especially the highly activated e-NPPs, which catalyze
Roshan M Borkar et al.
Journal of pharmaceutical and biomedical analysis, 102, 386-399 (2014-12-03)
Fidarestat, an aldose reductase inhibitor, has been used for the treatment of the diabetic associated complications such as retinopathy, neuropathy and nephropathy. To better understand the metabolism and pharmacokinetics of fidarestat, we have evaluated plasma protein binding, pharmacokinetics, tissue distribution
Reema Banarjee et al.
Journal of proteomics, 187, 69-79 (2018-06-24)
Endothelial dysfunction is one of the primary steps in the development of diabetes associated cardiovascular diseases. Hyperglycemic condition in diabetes promotes accumulation of advanced glycation end products (AGEs) in the plasma, that interact with the receptor for AGEs (RAGE) present
Fei Shen et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 1089, 1-7 (2018-05-09)
Liguzinediol (2,5-dihydroxymethyl-3,6-dimethylpyrazine, LZDO) is a potential agent for the low-risk treatment of heart failure. 2-N-acetylcysteine-LZDO (2-NAC-LZDO) and 2-cysteine-LZDO (2-Cys-LZDO) are major LZDO metabolites found in the pharmacokinetic studies of rats and beagle dogs. To elucidate the biotransformation pathway and related
Chun Yuan et al.
Molecular medicine reports, 16(4), 4529-4536 (2017-08-30)
Bone fracture healing is a complex process, which is associated with several factors, including age and osteoporosis. Certain genes and biological processes that may contribute to fracture healing, have been identified following developments in systems biology and molecular biology technologies
Wai Him Kwok et al.
The Journal of steroid biochemistry and molecular biology, 152, 142-154 (2015-06-03)
Androsta-1,4,6-triene-3,17-dione (ATD) is an irreversible steroidal aromatase inhibitor and is marketed as a supplement. It has been reported to effectively reduce estrogen biosynthesis and significantly increase the levels of endogenous steroids such as dihydrotestosterone and testosterone in human. ATD abuses
Aksorn Saengtienchai et al.
Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 214, 28-35 (2018-09-04)
There have been many reports regarding toxic chemicals in birds. Chemicals are mainly metabolized in the liver through phase I oxidation by cytochrome P450 (CYP) and phase II conjugation by conjugated enzymes, such as UDP-glucuronosyltransferase (UGT), sulfotransferase (SULT), glutathione-S-transferase (GST)
Ling Li et al.
Molecular cell, 80(3), 525-540 (2020-10-18)
Well-balanced and timed metabolism is essential for making a high-quality egg. However, the metabolic framework that supports oocyte development remains poorly understood. Here, we obtained the temporal metabolome profiles of mouse oocytes during in vivo maturation by isolating large number of
Bin Liu et al.
International journal of food microbiology, 337, 108927-108927 (2020-11-06)
Salmonella enterica serovar Enteritidis (S. Enteritidis) presents an excellent capacity to survive in egg white, which is a hostile environment for bacterial growth. To reveal its survival mechanism, this study focuses on the specific gene SEN1393, which has been found
Yuyuan Zhang et al.
Proceedings of the National Academy of Sciences of the United States of America, 111(32), 11612-11617 (2014-07-30)
During the early evolution of life, 8-oxo-7,8-dihydro-2'-deoxyguanosine (O) may have functioned as a proto-flavin capable of repairing cyclobutane pyrimidine dimers in DNA or RNA by photoinduced electron transfer using longer wavelength UVB radiation. To investigate the ability of O to
Sumit Bansal et al.
Journal of pharmaceutical and biomedical analysis, 120, 261-269 (2016-01-14)
Sulfotransferase 2A1 (SULT2A1) is a major catalyst of the sulfation of dehydroepiandrosterone (DHEA) to dehydroepiandrosterone sulfate (DHEA-S) in human liver cytosol. However, there is a lack of a sensitive and fast analytical method for the human liver cytosolic SULT2A1-dependent DHEA
You-Jin Kim et al.
Biological & pharmaceutical bulletin, 38(2), 218-227 (2015-03-10)
Sauchinone, a biologically active lignan found in Saururus chinensis (Saururaceae), exerts various biological activities against jaundice, inflammatory disease, hepatic steatosis, and oxidative injury. Despite its diverse applications, there exists some information about sauchinone's pharmacokinetics but its tissue distribution, metabolism, and
Feng Rao et al.
Biochemical and biophysical research communications, 398(3), 500-505 (2010-07-06)
The recent report of 2',3'-cAMP isolated from rat kidney is the first proof of its biological existence, which revived interest in this mysterious molecule. 2',3'-cAMP serves as an extracellular adenosine source, but how it is degraded remains unclear. Here, we
Tristan A Smythe et al.
Environmental science & technology, 51(12), 7245-7253 (2017-05-26)
The inhibitory effects of five novel brominated flame retardants, 1,2-bis(2,4,5-tribromophenoxy)ethane (BTBPE), decabromodiphenylethane (DBDPE), 2-ethylhexyl-2,3,4,5-tetrabromobenzoate (EH-TBB), bis(2-ethylhexyl)tetrabromophthalate (BEH-TEBP), and β-tetrabromoethylcyclohexane (β-TBECH), on thyroid hormone deiodinase (DIO) and sulfotransferase (SULT) activity were investigated using human in vitro liver microsomal and cytosolic bioassays.
Celine Gys et al.
Toxicology letters, 295, 115-123 (2018-06-18)
Bisphenol S (BPS) is increasingly used as substitute for bisphenol A, resulting in higher potential of human exposure to this compound. Yet, information on the human metabolism of BPS is limited. Hence, current biomonitoring studies rely only on the measurement
Hwa-Kyung Lee et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 1140, 121996-121996 (2020-02-06)
In this study, we performed the metabolism of endosulfan sulfate in human liver preparations (human liver microsomes, S9 fractions and hepatocytes) to identify new metabolites using liquid chromatography-high resolution mass spectrometry (LC-HRMS). Endosulfan sulfate is a major oxidized metabolite of
Jenny K Y Wong et al.
Drug testing and analysis, 8(2), 241-247 (2015-09-10)
The successful use of homogenized horse liver for the generation of phase I in vitro metabolites has been previously reported by the authors' laboratory. Prior to the use of homogenized liver, the authors' laboratory had been using mainly horse liver
Jiyoung A Hong et al.
Journal of medicinal chemistry, 52(17), 5485-5495 (2009-08-15)
Mycobacterium tuberculosis adenosine-5'-phosphosulfate (APS) reductase is an iron-sulfur protein and a validated target to develop new antitubercular agents, particularly for the treatment of latent infection. To facilitate the development of potent and specific inhibitors of APS reductase, we have probed
John W Nichols et al.
Environmental toxicology and chemistry, 40(1), 148-161 (2020-10-13)
The activity of a trout liver S9 substrate depletion assay has been shown to decline over time, presumably due to proteolytic degradation of biotransformation enzymes. To address this problem, assay performance was evaluated following the addition of phenylmethylsulfonyl fluoride (PMSF)
K M C Cornel et al.
Steroids, 139, 45-52 (2018-09-16)
Contradictory results are reported about the level of steroid sulfatase (STS), estrogen sulfotransferase (SULT1E1; together, the sulfatase pathway) and aromatase (CYP19A1) in endometrial cancer (EC). The aim of this study was to explore the levels of these enzymes in a
Edwin K Jackson et al.
The Journal of pharmacology and experimental therapeutics, 337(2), 444-450 (2011-01-29)
Studies show that kidneys produce 2',3'-cAMP, 2',3'-cAMP is exported and metabolized to 2'-AMP and 3'-AMP, 2'-AMP and 3'-AMP are metabolized to adenosine, 2',3'-cAMP inhibits proliferation of preglomerular vascular smooth muscle cells (PGVSMCs) and glomerular mesangial cells (GMCs), and A(2B) (not
Boontariga Wongsa et al.
Genomics, 112(1), 629-636 (2019-04-26)
The responsive mechanism of C. militaris TBRC7358 on xylose utilization was investigated by comparative analysis of transcriptomes, growth kinetics and cordycepin productions. The result showed that the culture grown on xylose exhibited high production yield of cordycepin on dry biomass.
Hua Bai et al.
PloS one, 15(5), e0231797-e0231797 (2020-05-05)
The pathological process and mechanism of myocardial ischemia (MI) is very complicated, and remains unclear. An integrated proteomic-metabolomics analysis was applied to comprehensively understand the pathological changes and mechanism of MI. Male Sprague-Dawley rats were randomly divided into a mock
Yang Yang et al.
Oncotarget, 8(25), 40289-40304 (2017-02-09)
Resveratrol (RV) is a natural polyphenol compound with a wide range of activities, including inhibition of human bladder cancer (HBC) cell growth. Because RV is rapidly metabolized and has poor bioavailability, it is unclear whether the antitumor activity is due
Jimmy Alarcan et al.
Toxicology letters, 307, 17-25 (2019-03-03)
13-Desmethylspirolide C (13-SPX-C) is a phycotoxin produced by dinoflagellates which can accumulate in shellfish. 13-SPX-C induces neurotoxic effects in rodents through blockade of nicotinic acetylcholine receptors. As no human intoxication has been to date attributed to the consumption of 13-SPX-C-contaminated
Edwin K Jackson et al.
Hypertension (Dallas, Tex. : 1979), 56(1), 151-158 (2010-06-03)
Recently we discovered that intact kidneys release into the extracellular compartment 2',3'-cAMP (a positional isomer of 3',5'-cAMP with unknown pharmacology) and metabolize 2',3'-cAMP to 2'-AMP, 3'-AMP, and adenosine. Because adenosine inhibits growth of vascular smooth muscle cells and mesangial cells
Manman Zhao et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 158, 105608-105608 (2020-10-31)
SYL927 and SYL930, two aminopropanediol analogues, are novel Sphingosine-1-phosphate receptor 1 (S1P1) modulators with higher selectivity and pharmacological activity compared with FTY720. Although the immunosuppressive activity of SYLs has been well demonstrated, information regarding the metabolic fates of the two
Hye-Jeong Hwang et al.
Colloids and surfaces. B, Biointerfaces, 173, 164-170 (2018-10-07)
Various phenol-containing molecules such as flavonoids have a wide range of biological effects including anticancer, antimicrobial, and anti-inflammatory properties, and, therefore, they have become subjects of active research for various medicinal and biological applications. To construct applicable materials incorporated with
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