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EZH can also interact with Ten
2022-01-03
EZH2 can also interact with Ten-Eleven Translocation gene family members (TET1, TET2, and TET3), which convert 5-methylcytosine (5 mC) to 5-hydroxymethylcytosine (5hmC), to cause changes in patterns of histone methylation and DNA methylation [52]. Huang et al. found that the expression levels of all
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The synthesis of substituted pyrimidinone carboxamides is ou
2022-01-03
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of Biotin-HPDP mg provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford insep
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In addition to indoles two
2022-01-03
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic PG 01037 dihydrochloride side chain to prepare compound (). The extension of
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The only approved H R
2022-01-03
The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or
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br Conclusion br Author contributions br Acknowledgements
2022-01-03
Conclusion Author contributions Acknowledgements We thank AMN-107 USC Center for Craniofacial Molecular Biology (CCMB) for their extensive guidance and teaching in biochemical techniques. We acknowledge Laurel Fisher, PhD for her contribution to statistical analysis of the data. We acknowle
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HO acted as an intracellular
2022-01-03
HO-1 acted as an intracellular defender against oxidative stress-induced cell damage. To elucidate the effects of HO-1 in ropivacaine-induced cytotoxicity in neuronal cells, HO-1 activity was inhibited using a specific HO-1 inhibitor zinc protoporphyrin, ZnPP. Our results indicate that ZnPP treatmen
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Introduction Cancer has been a significant public health pro
2022-01-03
Introduction Cancer has been a significant public health problem in the world with more patients being diagnosed every year. However, chemotherapy from non-specific cytotoxic agents that as an effective means of cancer treatment is limited by severe side effects and poor selectivity. Thus, the deve
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br Biochemical properties and post translational modificatio
2021-12-31
Biochemical properties and post-translational modification of GCAPs GCAPs are hydrophobic proteins that are likely permanently bound to their GC target under physiological conditions [5]. They interact with the photoreceptor GCs through the intracellular domains (reviewed in [17]). GCAP1 has been
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An interesting question is why
2021-12-31
An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino endothelin receptor antagonist mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequenc
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br Methods br Transfollicular penetration
2021-12-31
Methods Transfollicular penetration of herbs and their active constituents used for hair loss treatment The transfollicular administration of pharmacologically active molecules is recognised as a significant element for therapeutic interest, mainly with regard to delivery to specific sites of
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br Since viral infections result in polarization
2021-12-31
Since viral infections result in polarization of naïve CD4 T cells into both Th1 and Tfh subsets (although to variable degrees depending on the nature of the pathogen), a lot of effort has been devolved to the question of whether type I IFNs play a role in CD4+ T cell polarization. In vitro studie
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PBI is an agonist of GPR and acts as an
2021-12-31
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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Silodosin Limitations of our study are the
2021-12-31
Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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br The actions of GLP on the vasculature endothelium The
2021-12-31
The actions of GLP-1 (9–36) on the vasculature/endothelium The previous sections have ascribed the vascular and/or endothelial actions of GLP-1/GLP-1R agonists to potential direct actions through a canonical GLP-1R, but as mentioned previously, whether VSMCs and ECs express a full-length GLP-1R r
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The effects of GHS R a blockade on
2021-12-31
The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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