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The effects of the endocrine active
2021-08-05
The effects of the endocrine active agents on hepatic ERα were varied. Both nonylphenol and genistein caused an increase in hepatic ERα in female rats, whereas EE2 did not. It is doubtful that the small changes in hepatic ERα induced by genistein and nonylphenol in female rats are sufficient to alte
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br Cytokine impact on ILC fate Increasing evidence shows
2021-08-05
Cytokine impact on ILC fate Increasing evidence shows that ILC2 and ILC3 may convert into ILC1-like angiotensin receptor blockers by downregulating either GATA3 or RORγt, respectively, upregulating T-bet and gaining the capacity for IFN-γ production [60,61]. This process, often referred to as ‘I
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The TELI results of DNA damage
2021-08-05
The TELI results of DNA damage responses to CAA and SO then informed our choice of bacterial strains in subsequent experiments. We investigated E. coli cellular survival in response to CAA and SO exposure by determining the sensitivity of a number of E. coli strains, each possessing single or multip
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We found that both DDR
2021-08-05
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a rec
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Although it is believed that CYP
2021-08-04
Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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Compound was generated using a literature procedure
2021-08-04
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 chlorpromazine hydrochloride ). Hydroly
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We note that there are
2021-08-04
We note that there are slight qualitative differences among the similar time-optimal protocols. We attribute this to the challenging nature of our PDE and ODE state constrained optimization problem. While our optimization algorithm was able to converge to local optima in each case, it is likely that
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We have previously reported that CK is
2021-08-04
We have previously reported that CK2 is downregulated in senescent human lung fibroblast IMR-90 cells, aged rat tissues, and aging nematodes [17,18]. CK2 downregulation induces cellular senescence via the PI3K-AKT-mTOR-reactive oxygen species-p53-p21Cip1/WAF1 pathway in human cells [[19], [20], [21]
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In summary A is a potent orally available endothelin recepto
2021-08-04
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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For these reasons molecules of the
2021-08-04
For these reasons, molecules of the ET family and in particular ET-1 are considered useful factors in the evaluation of malignancy and in consequence, in the prognosis for several forms of neoplasia, such as ovarian (Bagnato et al., 2005), prostate (Nelson et al, 1995, Nelson et al, 1996), colorecta
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MuRF and MuRF in http www apexbt
2021-08-04
MuRF1 and MuRF3 in cooperation with the E2 ubiquitin-conjugating enzymes UbcH5a, -b, and -c were found to mediate degradation of myosin heavy chain β/slow (MHC β/slow) and MHC IIa via UPS, both, in vitro and in vivo [60]. Mice lacking both MuRF1 and MuRF3 developed skeletal muscle myopathy and hyper
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fty720 Herein the interactions of etamicastat nepicastat and
2021-08-04
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the fty720 exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains un
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br Development of the double strand break
2021-08-04
Development of the double strand break repair model for meiotic recombination Meiotic recombination was first described by Frans Alfons Janssens using Butaprost in the salamander Batracoseps attenuatus in 1909 [21] and then further elaborated at the genetic level in Drosophila by Thomas H. Morga
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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2021-08-04
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Given the excellent in vitro pharmacology profiles of methyl
2021-08-03
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic further information functionality of 1. Acetonitrile 49 was found to have a good balance of D
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