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br Results and discussion br
2019-10-10
Results and discussion Conclusion A new series of 2-mercapto-quinazolin-4-one analogues is designed and synthesized to possess electron withdrawing or donating functional groups (Cl or CH3O) at position 6- or 7-, 4-methoxyphenyl function at position 3. The 2-mercapto function is used to connec
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Furthermore we explored the effect of PKC
2019-10-10
Furthermore, we explored the effect of PKCζ on SIRT6 phosphorylation. Accumulating data showed that aPKC isoforms are involved in regulating lipid metabolism [41], [42], [43], [44], [45], [46], [47]. The aPKC activity was reported to play a dominant role in normal insulin signaling by activating PI3
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In contrast to AChE BuChE Table exhibited
2019-10-10
In contrast to AChE, BuChE (Table 2) exhibited a measurable time-dependent inactivation only with Fisetin clinical 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 greate
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In summary A is a
2019-10-10
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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There is a considerable molecular genetic heterogeneity with
2019-10-10
There is a considerable molecular genetic heterogeneity within ES/PNET. As mentioned above, either or can rearrange with in these gene fusions. Furthermore, for either gene fusion, additional heterogeneity stems from the location of the genomic breakpoints of the translocation, resulting in diffe
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br Conclusion From the series
2019-10-09
Conclusion From the series of synthesized N-methylated and N-benzylated pyrimidinediones, it may be concluded that the presence of electron rich species with pyrimidinediones is vital for enhancing binding with target, although, incorporation of steric bulky group must be taken into consideration
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Khan et al investigatedAnomalin a pyranocoumarin constituent
2019-10-09
Khan et al. investigatedAnomalin 44, a pyranocoumarin constituent of S. divaricata, which exhibits potent anti-inflammatory activity. The anomalin 44 dose-dependently inhibited inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) mRNA and protein expression in LPS-stimulated RAW 264.7
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Previously we have shown that complexes of
2019-10-09
Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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Enlarging the ligand binding pocket by reduction
2019-10-09
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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Furthermore elastase might not be the only
2019-10-09
Furthermore, elastase might not be the only regulator of CBG on cleaved and uncleaved form. In a study by Nenke et al. [85] α1-AT deficient subjects, who lack this native neutrophil elastase inhibitor, paradoxically have higher levels of uncleaved CBG and lower levels of CBG* [85]. Gender differenc
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It has only recently been appreciated that
2019-10-09
It has only recently been appreciated that antigen-activated coelenterazine mass undertake two additional transient migrations during the early stages of T-dependent antibody responses. In the first of these, antigen-activated B cells migrate rapidly (within 2–3h) to the outer regions of the follic
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br Introduction O Methylguanine DNA methyltransferase MGMT i
2019-10-09
Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic
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Ubiquitination is a reversible posttranslational modificatio
2019-10-09
Ubiquitination is a reversible posttranslational modification. The removal of Ub is carried out by enzymes known as deubiquitinases (DUBs). The antagonistic role played by these enzymes in the Ub pathway regulates the function of the ubiquitinated proteins, while maintaining the free Ub pool in euka
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We initially identified four putative Egr binding sites and
2019-10-09
We initially identified four putative Egr1 Reparixin kinase (−39/−36, −105/−102, −107/−104, and −227/−224) on the DBH proximal promoter. The deletion and mutagenesis experiments indicate that the motif at −227/−224 is required for Egr1-elicited reduction in DBH promoter activity. It remains to be d
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Acetazolamide Support for Cloninger s personality
2019-10-09
Support for Cloninger\'s personality theory comes also from molecular genetic studies. Given the high heritability of personality it is plausible that gene variants explain variance in RD. In Acetazolamide to endocrine studies, which relate hormone levels mostly in the periphery (blood, saliva, uri
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