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The effects of GHS R
2022-09-01

The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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So far several methods have been used
2022-09-01

So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute Fructose Colorimetric/Fluorometric Assay Kit slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels
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Clinical trials of all GSIs have ended prematurely raising t
2022-09-01

Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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br The potential of EPA
2022-09-01

The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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Barasertib Interestingly we have shown that OA required FFAR
2022-09-01

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 receptor binding assay used in
2022-09-01

The receptor binding assay used in our previous study demonstrated that propofol competitively binds to FPR1, thus blocking the downstream signal transduction of FPR1 and inhibiting neutrophil immune activities [8]. In this study, we assessed the pharmacological action of fMMYALF in the presence of
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Due to the presence of all FGFRs in the epithelium
2022-09-01

Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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Another lever to efficiently eradicate tumors including ovar
2022-09-01

Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing
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In this study according to the critical
2022-09-01

In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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Andexanet alfa works as a decoy for the
2022-09-01

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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Finally we investigated increasing basicity as a
2022-08-30

Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, Parthenolide demonstrated significant improvement of values of solubility for the two media, especiall
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Previous studies have demonstrated that cannabinoid
2022-08-29

Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xi
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However it is unclear whether the parent and transition
2022-08-29

However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic gonadotropin releasing hormone receptor will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs
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br Ghrelin Ghrelin was purified from rat stomach about twent
2022-08-29

Ghrelin Ghrelin was purified from rat stomach about twenty years ago as a 28-amino Sepantronium octanoylated peptide and shown to be the endogenous ligand of the growth hormone (GH) secretagogue receptor (now termed GHSR1a, Howard et al., 1996, Kojima et al., 1999). GHSR1a is a 7-transmembrane re
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Mdivi 1 Introduction br Alzheimer pathology A and Tau Amyloi
2022-08-29

Introduction Alzheimer pathology: Aβ and Tau Amyloid β protein (Aβ) plays an important role in AD pathogenesis. At the molecular level, senile amyloid plaques and neurofibrillary tangles (NFT) are two neuropathological hallmarks of AD [1]. Mutations in genes encoding amyloid precursor protein (A
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