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Dexamethasone DEX a potent synthetic glucocorticoid drug is
2020-06-30
Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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Three DDR binding sites have been mapped on
2020-06-29
Three DDR2 binding sites have been mapped on the collagen triple helix by us for collagen type 1 and by others using the collagen toolkit for collagen type 2. All of the three reported binding sequences are conserved in the α1 chain of collagen types 1, 2 and 3. The central motif sequence GARGQAGVMG
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The requisite extended benzyl alcohols
2020-06-29
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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From the general synthetic route we first synthesized a dire
2020-06-29
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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NVP-BKM120 To date little is known about mode of action or
2020-06-29
To date, little is known about mode of action or the underlying genetic basis of DEET repellency for human-biting ticks. To begin to unveil these mechanisms, we carried out behavioral assays to confirm the effectiveness of DEET as a deterrent for D. variabilis. RNA sequencing was then used to build
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br Methods br Results br Discussion Literature showed
2020-06-29
Methods Results Discussion Literature showed SN was well studied for its antigastric ulcer, antiinflammatory, antihyperglycemic, and antihyperlipidemic properties. Although a recent publication reported that SN was found to exert its regulatory effect in animal cholesterol levels, the exact
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Udenafil also has shown the ability to significantly inhibit
2020-06-29
Udenafil also has shown the ability to significantly inhibit the decrease of vascular endothelial cell function and inhibit the decrease in endothelial cell and smooth muscle contents, thus preventing their fibrosis within the penile corpus cavernosum in diabetic or hyperlipidemic animal models whe
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br Materials and methods br Results
2020-06-29
Materials and methods Results Discussion The effect of progestogen treatment showed some tendencies affecting the body length and weight, however these data were not verifiable statistically. This observation could be explained with the relatively short exposure period and/or the relatively
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Multi subunit RING type E ligases are exemplified
2020-06-29
Multi-subunit RING-type E3 ligases are exemplified by the CULLIN-RING-ligase (CRL) and the anaphase-promoting complex/cyclosome (APC/C) [19]. CRLs constitute the biggest family of other multi-component E3 ligases. These consist of a cullin scaffold protein (CULLIN 1, 2, 3, 4A, 4B, 5, 7), a substrate
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br Materials and methods br Results br
2020-06-29
Materials and methods Results Discussion We found that mRNA expression of PCNA significantly was down-regulated in BCP-ALL 2 deoxy d glucose australia following co-treatment with doxorubicin and NU7441 (Fig. 6e). Our result is congruent with Gehen et al. study reporting that down-regulation
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In summary our findings show that LPS can activate
2020-06-28
In summary, our findings show that LPS can activate CysLT2R on microglial carnosic acid to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of
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ARA metabolites which are produced through cytochrome
2020-06-28
ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic Dynorphin (2-17), amide, porcine (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and natureti
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br Conclusion In vivo pharmacokinetic
2020-06-28
Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokine
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Nearly years ago the first two enzymes
2020-06-28
Nearly 60years ago, the first two Alfacalcidol which catalyze the phosphorylation of proteins were discovered [1]. Protein phosphorylation was originally identified as a regulatory mechanism for the control of glycogen metabolism. Today it is clear that protein phosphorylation regulates most aspects
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br Agonist binding ETA activation is promoted
2020-06-28
Agonist binding ETA activation is promoted by binding of the endogenous peptidergic agonists to their orthosteric binding site on the receptor. ET1 and ET2 (Trp6-Leu7-ET1) bind with equal high affinity to ETA, whereas the third endogenous isopeptide ET3 (Thr2-Phe4-Thr5-Tyr6-Lys7-Tyr14-ET1) binds
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