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Since the initial identification of DNA
2020-03-04
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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br Concluding remarks A crucial step in the
2020-03-04
Concluding remarks A crucial step in the microbial degradation of steroids is the 1(2)-dehydrogenation of the steroid nucleus by FAD-dependent Δ1-KSTDs. This step is required to initiate the opening of the steroid nucleus under both aerobic and anaerobic conditions. A large variety of steroid-deg
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br Results and discussion br Conclusion Novel and
2020-03-04
Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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In these studies the inflammatory cytokine IL was
2020-03-04
In these studies, the inflammatory cytokine IL-8 was demonstrated as one of the responsible molecules induced by CysLTs via activating CysLT2 receptors. IL-8 is synthesized in and released from mononuclear cells, macrophages, fibroblasts and airway epithelial cells, and it promotes inflammation as a
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Cytochrome P CYP enzymes plays
2020-03-04
Cytochrome P450 (CYP-450) enzymes plays an essential role in pharmacology of drugs and toxicology of xenobiotics. Inhibition of these enzymes may lead to increase plasma levels of a concomitantly administered drug (Lee et al., 2013). It may prolong or reduce the pharmacological effects and increase
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In order to further evaluate cpt a function
2020-03-04
In order to further evaluate cpt1a function, we determined its tissue distribution in large yellow croaker. The mRNA levels of cpt1a were detected in all the tested tissues, but at varying levels. cpt1a mRNA expression was the highest in liver among different tissues, similar to reports in other fis
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A putative SHBG receptor SHBG R has been postulated for
2020-03-04
A putative SHBG Dioscin (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHBG is already bou
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Prenylation may turn a flavonoid from an
2020-03-03
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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Taken together our results demonstrate that the changes
2020-03-03
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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calcitriol hormone In contrast to AChE BuChE Table exhibited
2020-03-03
In contrast to AChE, BuChE (Table 2) exhibited a measurable time-dependent inactivation only with calcitriol hormone 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 gre
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In conclusion we demonstrated phenoconversion of CYP A
2020-03-03
In conclusion, we demonstrated phenoconversion of CYP3A in stable kidney transplant recipients, and that higher plasma indoxyl sulfate concentrations in these subjects may be involved in the phenomenon. The present findings suggest that dose adjustment of drugs metabolized by CYP3A may be needed in
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br Materials and methods br Results br Discussion In this
2020-03-03
Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel
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E protein was studied using specific anti E antibodies
2020-03-03
E1 protein was studied using specific anti-E1 Cy3 maleimide (non-sulfonated) in wild type cells and in transfected cells overexpressing the enzyme. The results revealed several unusual characteristics, which are unique to this ubiquitin-activating enzyme. The E1 was translated as a full-length prot
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br Materials and methods br Results br Discussion UPP
2020-03-03
Materials and methods Results Discussion UPP components including the proteasome, E1s, E2s, E3s and DUBs may become one the most important MG-262 australia of therapeutic targets for the pharmaceutical industry in the near future and supersede those which are involved in the phosphorylation
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From these and other studies it is clear that
2020-03-02
From these and other studies, it is clear that acriflavine is an interesting 3-Deazaadenosine with pleiotropic anticancer effects [21], [22], [43]. Its past systemic use in the clinical setting as an antibiotic without any major toxicity reported encourages further development of the drug for cance
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