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br Introduction Farnesoid X receptor FXR is a
2022-07-29
Introduction Farnesoid X receptor (FXR) is a bile CCCP regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that are invol
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Iloperidone receptor The highest metabolic stability observe
2022-07-29
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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Lenvatinib is an orally available multi targeted tyrosine
2022-07-29
Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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FLAG tag Peptide GPR which is also known
2022-07-29
GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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br Results and discussion CATALYST software allows automatic
2022-07-29
Results and discussion CATALYST software allows automatic pharmacophore construction by using a collection of molecules with activities ranging over a number of orders of magnitude. In addition, CATALYST pharmacophores (hypotheses) explain the variability of bioactivity with respect to the geomet
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Altiratinib br Materials and methods br
2022-07-29
Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka
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One year after the Brose paper was published Littleton
2022-07-29
One year after the Brose . paper was published, Littleton . reported the first measurements of evoked synaptic transmission in syt1 nulls, using the neuromuscular junction as a model system. These experiments revealed that syt1 was essential for rapid, robust evoked neurotransmitter release. Similar
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The combination of HIV antigen
2022-07-28
The combination of HIV antigen and antibody testing with the fourth generation immunoassays shortens the window fccp for HIV by detecting HIV antigen, which appears in the blood before seroconversion [3,5,11,12]. Analysis of the seroconversion panels indicated the Elecsys® HIV Duo assay has a good
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br Pharmacological anti aging approaches and the Hippo pathw
2022-07-28
Pharmacological anti-aging approaches and the Hippo pathway Aging and age-related pathologies are the main causes of disabilities and death. As Magalhañes and colleagues suggest, the challenges of developing anti-aging pharmacological therapies may, in part, be due to the complexity of aging mole
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br Conclusion br Introduction Gastric adenocarcinoma GA is
2022-07-28
Conclusion Introduction Gastric adenocarcinoma (GA) is the fifth most commonly diagnosed malignancy and the third most common cause of death due to cancer worldwide. It is a highly aggressive cancer and 5-year survival rate (5YSR) is usually 78 4 synthesis might be one of the critical biosynth
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br Materials and methods br
2022-07-27
Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin dexdomitor and functionally characterized the majority of the recept
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Continuing studies of endocannabinoid ligands at GPR reveal
2022-07-27
Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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In the present study we showed that reduced neuron formation
2022-07-27
In the present study, we showed that reduced neuron formation in vitro induced by IL-1β was ameliorated by activation of GPR55 in both human and mouse cultures of NSCs. Pre-treatment with GPR55 agonists also blocked upregulation of inflammatory cytokine receptor mRNA (IL-1R1, IL-6st) while increasin
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Further our study provides the first evidence that zaprinast
2022-07-27
Further, our study provides the first evidence that zaprinast and kynurenic cytochalasin d administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effective analg
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xanthine oxidase inhibitor Fig summarizes the underlying mec
2022-07-27
Fig. 7 summarizes the underlying mechanism of SB on inhibiting inflammation and maintaining epithelium barrier integrity in the TNBS-induced colitis model. Our findings not only explained the protective effect of SB on colon health, but also provided evidence that GPR109A likely constitutes a valid
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