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phospholipase a2 inhibitor In the present study we used lina
2020-12-25
In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma
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Addressing whether impaired activation of
2020-12-25
Addressing whether impaired activation of D1 and D2 receptors regulates memory capacity is relevant for all human pathologies that lead to reduced activation of these ezh2 inhibitor pathways, such as ageing [39], certain genetic polymorphisms [40] and neurodegenerative disorders. In this study, we
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Introduction Double strand break DSB is
2020-12-25
Introduction Double strand break (DSB) is the most deleterious damage that threats DNA integrity. This frequent damage arises from environmental stress like UV, chemical agents or ionizing radiations (IRs). Although environmental stress does not lead directly to DSB, it produces carboxypeptidase d
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br Common features of TdT pol and pol TdT pol
2020-12-25
Common features of TdT, pol μ and pol λ TdT, pol μ and pol λ remain in a closed conformation throughout their catalytic cycle, contrary to pol β [24•, 53, 54•]. One possible explanation for this observation is that they have traded fidelity (which requires open-to-closed transition) for a very ti
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Nowadays colorimetric assay has been applied in detecting DN
2020-12-25
Nowadays, colorimetric assay has been applied in detecting DNA MTase activity. Li et al. used DNA modified gold nanoparticles (AuNPs) coupled with enzyme-linkage reactions to detect the activity of methylases [20]. In a previous study, our group presented a label-free colorimetric method, using unmo
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Direct coupling between DNA methyltransferase
2020-12-25
Direct coupling between DNA methyltransferase enzymes and posttranslational modifications on histone proteins has been observed in mammals. For example, DNMT3A recognizes unmodified H3 through an ATRX-DNMT3-DNMT3L (ADD) domain, and its activity is inhibited by methylation of H3 at K4 (Li et al., 201
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Thus DGK active sites remain
2020-12-25
Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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Given the excellent in vitro pharmacology
2020-12-25
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic GSK256066 mg functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1
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br Results br Discussion Prostate cancer
2020-12-25
Results Discussion Prostate cancer dissemination and skeletal metastases represent major therapeutic challenges. Once the skeletal metastasis occurs, the incurable patient could just be symptomatically treated to alleviate the pain. Therefore it is of great necessity to disclose the molecular
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br Materials and methods br Results
2020-12-25
Materials and methods Results Discussion Conclusions First, we replicated the association of DDR1 with SZ in an independent Spanish sample and demonstrated that a SNP-SNP interaction within DDR1 played a role in the association with the disease. Second, we observed that SZ subjects with
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Cell migration and invasion are central
2020-12-25
Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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br Materials and methods Male
2020-12-25
Materials and methods Male Hartley guinea pigs (300–350g) were obtained from National Laboratory Animal Center, Taiwan. LTD4, LTC4, LTE4, LTB4, montelukast and BAY u9773 were purchased from Cayman Chemical, Ann Arbor, Michigan; Carbachol, atropine, l-serine, boric acid, l-cysteine and all buffer
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Apart from neutrophil mediated inflammation the production o
2020-12-25
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α prod
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A related cell based approach was used to
2020-12-25
A related, cell-based approach was used to test the functionality of the various HIV Rev fusions, but in a trans-complementation assay using 293T producers transfected with both VSV G and a Rev-deficient HIV reporter vector encoding both FFLUC and bsd (Fig. 2C). As expected, the non-fused, full-leng
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Compounds and were outliers for
2020-12-24
Compounds and were outliers for this equation being the two most reactive compounds. The presence of outliers implies that other factors or specific mechanisms are involved in their chemical hydrolysis. Generally urea derivatives prove to be highly stable in aqueous solutions in vitro. Additional
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