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We show that pharmacological inactivation of GSTP over a
2021-11-11
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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The experiments reported herein were
2021-11-11
The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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While the specific set of challenges associated with
2021-11-11
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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To apply the recently developed GPR ligands to
2021-11-11
To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the JIB-04 and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, the pre
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SR 8278 On the basis of their relative Glu transport rates
2021-11-11
On the basis of their relative Glu transport rates and anion currents, EAATs group into two functionally distinct classes, EAAT1–3 being efficient Glu transporters with small associated macroscopic anion currents and EAAT4–5 low-capacity transporters with predominant anion conductance [18]. The diff
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5-hme-CTP br Acknowledgments The financial support
2021-11-11
Acknowledgments The financial support from the National Natural Science Foundation of China (Nos. 31460422 and 31060210), the Natural Science Foundation of Jiangxi Province, China (20171BAB204029 and 20143ACB20006), the Project of Science and Technology of Jiangxi Provincial Education Department,
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Limitations of our study are the following we
2021-11-11
Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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A key limiting factor in the
2021-11-11
A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of Dextran sulfate sodium salt receptor of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24
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br Conclusions Temporally controlled disruption of
2021-11-11
Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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As early as glucagon was shown to
2021-11-11
As early as 1957, glucagon was shown to increase chemical d expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27]. This
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To further investigate if GPR was
2021-11-11
To further investigate if GPR40 was the functional target of these phenylpropiolic Cyprodime hydrochloride synthesis analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium
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Both anxiety like behavior and sucrose preference intake
2021-11-11
Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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br Molecular mechanisms and pathways for ferroptosis
2021-11-11
Molecular mechanisms and pathways for ferroptosis regulation As to the regulation of lipid peroxidation, iron and related ROS metabolism involved in ferroptosis, many molecular mechanisms and pathways have been presented. It is generally believed that cystine/glutamate antiporter system Xc−, GPX4
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br Funding The authors disclose the following support for
2021-11-11
Funding The authors disclose the following support for the research and/or authorship of this article: This work was supported by the Canadian Institutes for Health Research (CIHR). TM is the recipient of a BMS/CTN postdoctoral fellowship and PKQ was funded by a CAHR/CIHR doctoral scholarship. A
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Clonidine HCl australia Not all metals are susceptible of be
2021-11-10
Not all metals are susceptible of being accumulated by insects. Tissue concentrations of essential metals like Cu and Zn are regulated in many insects and hence cannot be used to biomonitor metal pollution (Hare, 1992). A similar behaviour could explain the observed stability of Zn and Cu relative t
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