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KB SRC 4 br Materials and methods br Results
2020-03-24
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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Therapeutic options targeting intrahepatic resistance are ve
2020-03-24
Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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br Materials and methods br
2020-03-23
Materials and methods Results Among 17,061 probes, the Plumbagin mg of 758 probes (4.4%) showed at least a 2-fold upregulation (230 probes) or downregulation (528 probes) at day 3 after VMH lesioning as compared with sham-VMH lesioning. Supplement Table 1 shows the upregulated (>2-fold) and t
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Interestingly all three lesions that significantly inhibited
2020-03-23
Interestingly, all three lesions that significantly inhibited transcription – CPD, εA and the AP site, – promoted insertion of MK-1775 residues opposite the damaged nucleotide. Thus, bacterial RNAP seems to follow the so-called ‘A-rule’ for incorporation of nucleotides opposite AP-sites and bulky le
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br Deregulation of CDK Many
2020-03-23
Deregulation of CDK5 Many neurotoxic or stress conditions like ischemic mitotic inhibitors damage, oxidative stress, mitochondrial dysfunctions, excitotoxicity, Aβ exposure lead to disruption of the tight regulation of Cdk5 (De Strooper et al., 2010). Calpain-mediated cleavage of p35 to p25 is a
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Acknowledgements This work was supported in part by
2020-03-23
Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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Currently approved anti obesity drugs for long term
2020-03-23
Currently approved anti-obesity drugs for long term use such as orlistat, lorcaserin and liraglutide are efficient in reduction of weight gain but are limited in usage due to their adverse effect profile and higher cost (Krentz et al., 2016; Mopuri and Islam, 2017). In Chlorocresol receptor to this
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Mass spectrometry has previously been used to examine
2020-03-23
Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino egfr inhibitor analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, however
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In summary we hypothesize that targeting the
2020-03-23
In summary, we hypothesize that targeting the A1R–D1R heterotetramer with heteromer-selective drugs might improve safety and efficacy of the pharmacological therapy for RLS and other motor diseases, resulting in fewer side effects than classical drugs developed for targeting monomeric A1R or D1R.
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More recent studies have correlated
2020-03-23
More recent studies have correlated sPLA2-V with alternative macrophage activation (M2) in human and murine macrophages [149,150]. sPLA2-V expression was induced during both human and mouse interleukin-4–mediated activation of macrophages in vitro, and its absence impaired macrophage activation in v
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palovarotene br Introduction Analyses of genomic alterations
2020-03-23
Introduction Analyses of genomic alterations in cancer have identified epidermal growth factor receptor (EGFR) as one of the most potent “oncogenic driver” kinases that is present in many epithelial tumors including endometrial, breast, prostate, skin, esophagus, lung, stomach, colorectal, and re
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Our structures also provide new insights
2020-03-23
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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(+)-Usniacin Interestingly all three lesions that significan
2020-03-21
Interestingly, all three lesions that significantly inhibited transcription – CPD, εA and the AP site, – promoted insertion of (+)-Usniacin residues opposite the damaged nucleotide. Thus, bacterial RNAP seems to follow the so-called ‘A-rule’ for incorporation of nucleotides opposite AP-sites and bu
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Although the formation and toxicity of DPC is
2020-03-21
Although the formation and toxicity of DPC is theoretically acceptable, it is difficult to evaluate the specific role of DPC and its repair enzyme MGMT in the cytotoxic and mutagenic effects because DPCs are estimated to constitute only 1%–3% of total DNA damage when Tanshinone IIA---sulfonic sodium
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br Conclusions The PQQ dependent
2020-03-21
Conclusions The PQQ-dependent CcPDH is the first PQQ-dependent enzyme identified in eukaryotes. The PQQ cofactor binds the enzyme with high affinity, reflected in a Kd of 1.1 nM, and the enzyme oxidizes 2KG, l-fucose, and rare sugars such as d-arabinose and l-galactose. The AA8 cytochrome b domai
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