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Despite the sources of error discussed above
2020-04-10
Despite the sources of error discussed above, several trends have emerged and much valuable data are available regarding binding affinities of progestogens for different steroid receptors. All the progestogens bind to the PR with a high affinity, typically in the nanomolar range. For example the syn
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Determination of relative potency EC by
2020-04-10
Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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br Acknowledgements br Introduction L Rhamnosidases
2020-04-10
Acknowledgements Introduction α-L-Rhamnosidases (EC 3.2.1.40) are glycosyl hydrolases (GHs) that cleave terminal α-l-rhamnose from a large number of natural products [1]. The action of α-L-rhamnosidases (α-RHAs) has been reported, among others, on different complex substrates such as heteropol
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Third DGK protein stabilization by myristic acid is cell lin
2020-04-10
Third, DGKδ2 protein stabilization by myristic cycloheximide solubility is cell line specific. Myristic acid had no obvious effects on DGKδ protein stability in the liver cell line HepG2, pancreas cell line MIA-PaCa-2 and neuronal cell line Neuro-2a cells (Fig. 5). Although myristic acid moderately
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Another important mediator in fear learning is
2020-04-09
Another important mediator in fear learning is the neuropeptide corticotropin-releasing factor (CRF). For example, local repeated administration of CRF into the basolateral amygdala potentiates the acquisition of cue-conditioned fear (Bijlsma et al., 2011) and CRF1 receptor antagonists effectively b
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A recent study reports the expression of glutathione depende
2020-04-09
A recent study reports the expression of glutathione-dependent enzymes (GGT, GST-isoforms, gamma-glutamylcysteine synthetase, glutathione disulfide reductase and GSH peroxidase) in human primary PT interleukin in four subsequent passages [33]. In this study, we present phase I and II activities at
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br Molecular modeling study Molecular modeling
2020-04-09
Molecular modeling study Molecular modeling study was essentially needed to understand and interpret the DHFR inhibitory pattern of this new class of compounds. Computational docking is an algorithm designed to estimate two main terms. The first is to determine the suitable position and the orien
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The acid base properties of
2020-04-09
3. The acid-base properties of the IL are important issues to consider because protonation changes caused by Brønsted-acidic or basic ions may result in enzyme deactivation [29]. Thereby, the acid-base properties of the newly designed IL need proper control for enzymes by selection of appropriate ca
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How does an increase in
2020-04-09
How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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Another interesting finding regarding substrate selectivity
2020-04-09
Another interesting finding regarding substrate selectivity of iPLA2-VIA in whole cellular systems stems from the observation that some of the major species hydrolyzed by the enzyme contain a 16:1 fatty mmae at the sn-2 position [57,119], raising the possibility that iPLA2-VIA may constitute a majo
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Dual inhibition of ACE and NEP as a
2020-04-09
Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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br Materials and methods br Results br Discussion In
2020-04-09
Materials and methods Results Discussion In rodent species, CYP2E1 and CYP2B have been implicated in CCl4 metabolism. In this study, we used expressed human CYP2E1 to show that this enzyme is a high-affinity catalyst responsible for low-dose CCl4 metabolism. Studies employing an inhibitory
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A decrease in heme levels enables the phosphorylation of eIF
2020-04-09
A decrease in heme levels enables the phosphorylation of eIF2α by HRI and thereby inhibition of eIF2α activity. Indeed, the relatively small change in cytosolic heme levels in SZ geldanamycin showed downstream functional consequences manifested by almost 50% elevation in the phosphorylation of eIF2
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br Conclusions This report describes the discovery
2020-04-09
Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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133 2 Several evidences showed that seizures increase brain
2020-04-09
Several evidences showed that seizures increase brain extracellular glutamate, which binds to N-methyl-d-aspartate (NMDA) receptor, then up-regulated cyclooxygenase-2 (COX-2) expression in brain capillaries to increase BBB P-gp expression [11,13,29,30]. A recent study demonstrated a different signal
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