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Our study revealed elevated basal Akt phosphorylation in die
2020-11-02

Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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There is evidence that the response of CYP
2020-11-02

There is evidence that the response of CYP450 activity to DEX is species-specific. CYP1A and CYP3A expressions were strongly induced by DEX in porcine hepatocytes (Rasmussen et al., 2014) and in rat and human, but not minipig or beagle dog hepatocytes (Lu and Li, 2001). Within fish, there are also
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br Results br Discussion Mucosal barriers
2020-10-31

Results Discussion Mucosal barriers are constitutively challenged by various stimuli, and the homeostasis of mucosal barriers both at steady state and upon challenge are maintained by tissue-resident immune Fmoc-Ser(tBu)-OH sale (Kurashima et al., 2013, Okumura and Takeda, 2016). ILC3s are fo
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Like all other cellular processes ubiquitination is also tig
2020-10-31

Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con
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br Molecular modeling study Molecular modeling
2020-10-31

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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DDI is one of the main
2020-10-31

DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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Introduction Cytochrome P CYP A is the most important
2020-10-31

Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The This means level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A m
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In contrast to AChE BuChE Table exhibited
2020-10-31

In contrast to AChE, BuChE (Table 2) exhibited a measurable time-dependent inactivation only with 23401 zip code sale 2 among the four acetophenones in this study. Values of Ki obtained from steady-state inhibition of BuChE by all four acetophenones were, as noted in the Results, 10- to 200-fold gr
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Determination of relative potency EC by dose response assays
2020-10-31

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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Recently experimentally exposed common carp took up CLO from
2020-10-31

Recently, experimentally-exposed common carp took up CLO from water and maintained a consistent concentration in the liver and blood plasma (Corcoran et al., 2014). Clotrimazole may influence other aquatic organisms. Survival and development of marine shrimp larvae (Palaemon serratus) were affected
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Consistent with a clear separation of biological function
2020-10-31

Consistent with a clear separation of biological function between ARISC and BRISC in cells, mutations in BRCC36 and Abraxas are prevalent in cancer genomes whereas mutations in KIAA0157 are rare. A survey of the Catalogue of Somatic Mutations in Cancer (COSMIC) consortium, revealed that to date, 37
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Mitochondrial depolarization induced by DHODH inhibition Fig
2020-10-31

Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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Almost of drugs in the market undergo deactivation though
2020-10-30

Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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Similarly EGCG restored the mitochondrial energy shortfall i
2020-10-30

Similarly, EGCG restored the mitochondrial energy shortfall in fibroblasts and lymphoblasts of the patients affected by Down syndrome, even so the mechanism of the effect was not clearly known (Valenti et al., 2013). EGCG also stimulated the mitochondrial biogenesis by activation of nuclear respirat
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br Target enzyme attributes and substrate peptide selection
2020-10-30

Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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