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Compound was generated using a literature procedure and requ
2020-11-19
Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to wee1 inhibitor ). Hydrolysis of all methyl
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Multiple lines of evidence now indicate that mitochondrial d
2020-11-19
Multiple lines of evidence now indicate that mitochondrial decay is a fundamental factor that leads to alterations in energy metabolism in the aged heart (Hagen et al., 2002, Judge and Leeuwenburgh, 2007, Lesnefsky et al., 2001c). Nevertheless, the exact biochemical events that cause such an alterat
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The enzymatic activity of recombinant sponge P H was assayed
2020-11-19
The enzymatic activity of recombinant sponge P4H was assayed in vitro both at 37°C, the standard enzymatic kinetics temperature, and at 15°C, the typical sea temperature of C. reniformis marine environment (Fig. 2C). Surprisingly the data obtained indicate that the sponge enzyme has a lower activity
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br Materials and methods br Results and discussion
2020-11-19
Materials and methods Results and discussion Conclusions In this study, we have investigated the possibility that hierarchical phosphorylation by CK2 may play a role in cellular signal transduction. Hierarchical phosphorylation by CK2 requires multiple consensus determinants with specific s
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GW3965 HCl In the particular case of metals several
2020-11-19
In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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Measurement of Chol absorption synthesis and catabolism
2020-11-19
Measurement of Chol absorption, synthesis and catabolism would be very helpful to determine the underlying cause of hypercholesterolemia in individual patients at risk for atherosclerosis. The information could help to determine the best therapeutic approach to reduce Chol absorption, to reduce Chol
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In cholesterol synthesis HMG CoA reductase is
2020-11-19
In cholesterol synthesis, HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins or HMG-CoA reductase inhibitors are commonly used for management of hypercholesterolemia. The presence of an HMG-like moiety on these drugs allows them to competitively bind to the catalytic do
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AI-10-49 br Most reported binding data are obtained
2020-11-19
Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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Some authors rather than using
2020-11-18
Some authors, rather than using magnetic NPs as heat sources, have enhanced the activity of the linked enzymes by applying low frequency AMF. Magnetic energy is converted into a rotational motion of the enzyme-particle system that increase the collision rate with the substrate [14], [15], or trigger
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The activity of cysteine endopeptidases involved in the germ
2020-11-18
The activity of cysteine endopeptidases involved in the germination of caryopses is generally regulated at two levels: the hormonal induction of synthesis by gibberellins (Drzymała et al., 2008) and a putative regulation of activity by phytocystatines (Kiyosaki et al., 2007, Martinez et al., 2009),
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br Results br Discussion Taking advantage of the highly spec
2020-11-18
Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate hypoxia inducible factor that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2
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Cyclin D inhibits the transcriptional activity of the transc
2020-11-18
Cyclin D1 inhibits the transcriptional activity of the transcription factors myogenin and MEF2 [39,40]. In addition, myogenin activates MEF2 expression, which feeds back to amplify the myogenin promoter [38]. In this study, DGKδ suppression, in addition to the increase of cyclin D1, inhibited myogen
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The only reported synthesis of the aminobicyclic core
2020-11-17
The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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br Conclusion The results of the present
2020-11-17
Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by Cys
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In untreated rodent or human hepatocytes PXR or CAR
2020-11-17
In untreated rodent or human hepatocytes, PXR or CAR is stabilized by cytoplasmic co-chaperone partners like heat shock protein 90 (HSP90, Fig. 1). Upon ligand binding, the nuclear receptors are freed and translocated into the nucleus, identified as a pivotal step in PXR- or CAR-mediated transactiva
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