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Previous studies revealed the expression of the CCR receptor
2020-01-03
Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr
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Compound was prepared from chloroindole by acylation to
2020-01-03
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole Hoechst 34580 derivative (). Derivatives and we
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Our results demonstrated that ET a
2020-01-03
Our results demonstrated that ET-1, a Wnt ligand, stimulated the Wnt/β-catenin signaling pathway. First, ET-1/ETRA binds to Frizzled family cell-surface receptors, resulting in the activation of Dvl1, a Dishevelled (DSH) family protein. Next, activated DSH inhibits the Axin, GSK-3β, and APC protein
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In this regard http www apexbt
2020-01-02
In this regard, some attempts have been made to reduce the presence of those radicals. In presence of fluorine source, it seems that the fluorine atoms can substitute the hydrogen atoms linked to silicon atoms, forming Si-F bonds with a higher bonding GTP-Binding Protein Fragment, G alpha (536 kJ mo
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Intriguingly one E residue may serve as a molecular gate
2020-01-02
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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Similarly synthetic analogs of Alogliptin by replacing the
2020-01-02
Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in
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The methods for DNA MTase activity assay involve radioactive
2020-01-02
The methods for DNA MTase activity assay involve radioactive labelling [15], gel electrophoresis [16], high-performance liquid chromatography [17], [18], bisulfite conversion [19], [20], and affinity enrichment [21], [22]. In these methods, the methylated bases under the action of active MTase could
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Alfacalcidol mg We next focused our design
2020-01-02
We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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Carbazole could be recrystallised from
2020-01-02
Carbazole could be recrystallised from ethyl acetate to provide bright red crystals suitable for single crystal X-ray diffraction (see ). The first crop showed had crystallised preferentially as the ()-isomer (A). Examining the single crystal X-ray data of it was interesting to find that the N2C1
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P falciparum DHFR TS is a particularly important enzyme
2020-01-02
P. falciparum DHFR-TS is a particularly important enzyme, because it is from the protozoan species that is associated with most malaria infections. Since this enzyme is responsible for catalyzing sequential reactions in the thymidylate cycle, its inhibition slows malarial dTMP production and therefo
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PKI-402 Park et al expanded their own model as hydrogen bond
2020-01-02
Park et al. [34] expanded their own model as hydrogen- bonding lattice fluid EOS (NLF-HB) [35] for calculating the activity coefficients of aqueous amino PKI-402 solution. Further, Pazuki et al. [36] extended the perturbed hard chain theory which has been proposed by Beret and Prausnitz [37] for mo
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blue nitro In order to validate the ATP competitive mode of
2020-01-02
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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Increasing age among middle aged
2020-01-02
Increasing age among middle-aged subjects (30–59years old) was associated with higher levels of cholesterol synthesis markers (although without statistical significance) and also of cholesterol Tipiracil hydrochloride markers (with statistical significance for campesterol and sitosterol); this find
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Introduction Cognitive impairment is a core stable feature o
2019-12-31
Introduction Cognitive impairment is a core, stable feature of schizophrenia that limits patient functioning and well-being (Keefe and Harvey, 2012) and associates with poor functional outcome (Fervaha et al., 2014, Kontaxaki et al., 2014). Studies also indicate that cognitive deficits occur prior
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We also discovered important clues to
2019-12-31
We also discovered important clues to domain GW2580 of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs. Al
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