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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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In addition to an action via
2020-04-08

In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se
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Data from our in vitro studies
2020-04-08

Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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In normal cells the apoptotic stimuli lower the expression l
2020-04-08

In normal cells, the apoptotic stimuli lower the expression level of antiapoptotic proteins by increasing turnover rate and preventing the constant degradation of proapoptotic proteins. Thus, the dysregulation of anti-/pro-apoptotic proteins will confer the survival of cancer osi sc 175 via enhancin
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OHC is a potent regulator of LXR mediated
2020-04-07

25-OHC is a potent regulator of LXR-mediated pathways, that impact on Telenzepine dihydrochloride lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-O
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