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Cytochromes P CYP are a superfamily of hemoproteins
2019-12-03
Cytochromes P450 (CYP 450) are a superfamily of hemoproteins containing a heme cofactor, which are widely distributed in animals, plants and microbes (Hannemann et al., 2007). CYP450 exhibits a variety of biological functions including biotransformation of drugs, detoxification of endogenous and xen
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In a study on the time course of a mechanism
2019-12-03
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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As compared with the broad spectrum of chemicals
2019-12-03
As compared with the broad spectrum of chemicals known to serve as the ligands for PXR and CAR, the ligands of VDR are previously restricted to VD3 as well as its hydroxylated metabolites and the secondary bile bapta am sale LCA. Recently, the VDR-binding capacities of more compounds have been disc
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Deregulated Wnt signaling either due to pathway mutations or
2019-12-03
Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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In conclusion this study indicated
2019-12-02
In conclusion, this study indicated that D. tripetala and A. melengueta extracts inhibited CYP 3A enzyme both in vitro and in vivo. Although these inhibitions may appear to be weak from the US FDA classification point of view, caution must be applied in the concurrent use of herbal preparations cont
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Overall the evidence and the results from
2019-12-02
Overall, the evidence and the results from in vivo studies clearly indicate that cyclosporine biotransformation can be induced by dasatinib co-administration through induction of CYP3A expression. However, further studies are needed to explore the role of P-gp modulation in DDIs. Conclusion In v
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Muscle Ring Fingers MuRFs comprising TRIM MuRF TRIM
2019-12-02
Muscle Ring Fingers (MuRFs) comprising TRIM63 (MuRF1), TRIM55 (MuRF2) and TRIM54 (MuRF3) are the most studied TRIMs in the heart. However, with increasing knowledge of E3 ligases and recent advancements in the field, many other TRIMs such as TRIM8, TRIM21, TRIM24, TRIM32, TRIM45, TRIM69 and TRIM72 w
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indole 3 butyric acid Enzymatic assay The usual in vitro tes
2019-12-02
Enzymatic assay. The usual in vitro test for the measure of the activity of DbH involves ascorbate as a cosubstrate (e.g., 5mM) and tyramine as a substrate (e.g., 10mM). When using N-aryl-N′-hydroxyguanidines instead of ascorbate, the hydroxylase activity of DbH was measured by HPLC as the amounts o
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This hydrophobic biphenyl tail gave good binding affinity
2019-12-02
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC corresponding ZLN005 receptor was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding inte
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Introduction DHFR is an important enzyme in
2019-12-02
Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic apply for conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of t
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br Enzymes involved in microbial steroid degradation
2019-12-02
Enzymes involved in microbial steroid degradation are generally not expressed constitutively, but they are upregulated depending on which steroid substrates are present [17,81]. Thus, a cell-free extract prepared from testosterone-adapted C. testosteroni ATCC 11996 cells displayed a 1(2)-dehydroge
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The purposes of this study is to develop
2019-12-02
The purposes of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs using S-hexyl GSH, and to clarify the mechanism underlying response to such trapping using montelukast, a CysLT1 receptor antagonist, BayCysLT2RA, a CysLT2 recepto
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CDK lacks DNA binding domains and nuclear localization
2019-12-02
CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PAX
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Conversely to the reduction in restraint evoked HR increase
2019-12-02
Conversely to the reduction in restraint-evoked HR increase following the blockade of CRF receptors, Nijsen et al. [28] demonstrated that BNST treatment with a nonselective CRF 57 9 antagonist enhanced the tachycardia evoked by contextual fear conditioning. Taken together, these results indicate tha
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br Conclusion and future perspectives LDL
2019-12-02
Conclusion and future perspectives LDL cholesterol-lowering therapy is essential for cardiovascular risk reduction. On the background of a high inter-personal variation of cholesterol synthesis and cholesterol UK 356618 sale the efficacy of cholesterol lowering, both, with statins and with ezetim
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