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br Medium to long chain
2021-12-14

Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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High lipophilicity of seems to cause
2021-12-14

High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i
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Results of studies on fish FBPase are
2021-12-14

Results of studies on fish FBPase are somewhat confusing: although fishes skeletal muscles possess relatively high FBPase activity (Knox et al., 1980, Lushchak et al., 2001) and the isozyme present therein has kinetic properties typical to all vertebrates muscle FBPases (Rosenmann et al., 1977), inv
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Eribulin mesylate synthesis In hypoxic breast cancer cells
2021-12-13

In hypoxic breast cancer cells, BNIP3-mediated autophagy activation and elevation of amino Eribulin mesylate synthesis levels were notable. BNIP3, a BCL-2 family protein, is known to be transcriptionally regulated by HIF-1α and to be involved in cancer cell death in hypoxic conditions [51]. As a li
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Importantly recent in vivo results demonstrated
2021-12-13

Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla
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Targeting MCTs is likely to have
2021-12-13

Targeting MCTs is likely to have dramatic effects on lactate-dependent metabolic symbiosis described in the previous paragraphs. A plethora of MCT inhibitors have been described, including α-cyano-4-hydroxycinnamate (CHC) [59], organomercurials [60], stilbene disulfonates [60], and other second-gene
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br Results and discussion br Conclusions In summary
2021-12-13

Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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The relationship between increased GPR
2021-12-13

The relationship between increased GPR120 expression in the EDL skeletal muscle and systemic glucose control is yet to be investigated. However, if the increased expression of GPR120 correlates with enhanced insulin-stimulated glucose uptake in skeletal muscle, particularly the EDL muscle, this migh
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The occurrence of MDR in cancer
2021-12-13

The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer nor-NOHA acetate in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including
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The genes for the receptors for
2021-12-13

The genes for the receptors for peptides similar to glucagon are dispersed on three human chromosomes, with two on chromosome 17 (GCGR and GLP2R) and one each on chromosomes 6 (GLP1R) and 19 (GIPR) (see Table S1). The exon–intron gene structures of these genes are similar, as are the genes for other
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The molecular nature of these putative Ca channels is at
2021-12-13

The molecular nature of these putative Ca2+ antioxidants is at present unknown. Apart from the NSVDC channel, which is permeable to Ca2+ [27], [15] functional Ca2+ channels have been identified in patch clamp experiments [28]. These channels, which were characterized as B-channels, seem to have ver
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Among sensitizers tested in the previous
2021-12-13

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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br Competing interests br Authors contributions br
2021-12-13

Competing interests Authors contributions Transparency document Introduction Non-alcoholic fatty liver disease (NAFLD) is a spectrum of liver diseases ranging from simple steatosis to non-alcoholic steatohepatitis (NASH), which may further progress to liver cirrhosis and liver carcinoma
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In summary the SAR of
2021-12-13

In summary, the SAR of a series of phenylpropanoic acid-free fatty hmg-coa reductase receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robu
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In this study we followed the fate
2021-12-13

In this study, we followed the fate of Ag-specific CD8+ T URB597 by directly visualizing them using MHC class I tetramers coupled with ovoalubumin (OVA)257–264 following EG.7 inoculation. We also examined the mechanism of apoptosis in exhausted Ag-specific CD8+ T cells during tumor immune response
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