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Interestingly we have shown that OA required
2021-09-09

Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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The ultimate success of multimodal probe in the inflammation
2021-09-09

The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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FPR activation stimulates multiple signal transduction pathw
2021-09-09

FPR1 activation stimulates multiple signal transduction pathways responsible for various neutrophil functions, such as adhesion, chemotaxis, phagocytosis, adefovir of secretory granules, and superoxide anion radical (O2) production, which contribute to the physiological inflammatory response associ
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So what makes a FFAR agonist different and
2021-09-09

So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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Phleomycin synthesis Although drug monitoring is not usually
2021-09-09

Although drug monitoring is not usually requested, there are some cases where measurement of DOACs in Phleomycin synthesis is useful, and of special help for managing patients at risk. These cases include the control of adherence to a therapeutic protocol, surveillance of drug accumulation risk in l
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br Materials and methods br Results
2021-09-09

Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa Nourseothricin sulfate to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in t
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br Author contributions br Declaration of conflict
2021-09-09

Author contributions Declaration of conflict of interest Acknowledgements We are grateful to the Director, National Institute of Immunology for his support. The work was partially supported by J.C. Bose Fellowship to SSM. We acknowledge the help from staff of Small Animal Facility of Nation
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The glycolytic activator phosphofructo kinase fructose bisph
2021-09-09

The glycolytic activator 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase 3 (PFKFB3) is well-known as a downstream substrate of hypoxia-inducible factor 1α (HIF-1α) signaling pathway [5,6]. Tumor hypoxia has long been associated with increased malignancy, poor prognosis and drug resistance. HIF-
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In an attempt to gain increased molecular insights into
2021-09-08

In an attempt to gain increased molecular insights into in vivo transmigration of neutrophils, we applied an aseptic inflammatory skin chamber model. In this model, recruitment of neutrophils is typically associated with phenotypic changes of many plasma membrane localized adhesion receptors in peri
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We have previously established the pharmacokinetic
2021-09-08

We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in 5ht and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound CID in
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With the administration of OM fatty acids it has
2021-09-08

With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also de
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GPR is a member of the G protein
2021-09-08

GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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Selective pharmacological inhibition of tonic
2021-09-08

Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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The synthesis of is shown in
2021-09-08

The synthesis of is shown in . The ---Boc--diaminopropanoic acid--butyl ester () fragment was synthesized in four steps from Boc--asparagine (). The key step in this synthesis was a Hofmann rearrangement of the terminal carboxamide, which was performed according to the elegant protocol of Zhang that
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br Results br Discussion ER and GR play opposite
2021-09-08

Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in
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