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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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Of the acidic hydroxyazoles involved
2019-10-09
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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br Molecular modeling study Molecular modeling study was ess
2019-10-09
Molecular modeling study Molecular modeling study was essentially needed to understand and interpret the DHFR inhibitory pattern of this new class of compounds. Computational docking is an algorithm designed to estimate two main terms. The first is to determine the suitable position and the orien
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leukotriene receptor antagonists In this study we also condu
2019-10-08
In this study, we also conducted an analysis comparing the expression profiling of Hh genes among the sarcomas investigated. In these tumors, the IHH gene showed a higher expression level than PTCH1 gene in RMS and SS samples (pleukotriene receptor antagonists in human RMS cell lines as well as mous
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EP EP and EP receptor expression
2019-10-08
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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STF-62247 pathway To provide a brief critical
2019-10-08
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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