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In the present study five Glu
2022-09-09
In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Ghrelin readily crosses the blood brain
2022-09-09
Ghrelin readily crosses the blood AH 7614 barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al., 2011, Schele et al., 2016, Skibicka et al.,
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Knock out mice of FXR showed enhancing cholesterol
2022-09-09
Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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Macrocycle was synthesized as described in Under SAr
2022-09-09
Macrocycle was synthesized as described in , . Under SAr conditions, 2-chloronicotinonitrile was heated with -butyl 5-aminopentanoate in refluxing ethanol (). The resulting aminopyridine was treated with mesyl chloride and the nitrile was subsequently reduced to afford amine . Chloroaminopyrimidin
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This crosstalk may be responsible for the
2022-09-08
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on fluvoxamine maleate australia pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation
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The eel and perhaps other
2022-09-08
The eel, and perhaps other euryhaline teleost fish, have the additional peptide, renoguanylin that exhibits high levels of expression within the kidney as well as the intestine. In terms of overall sequence, pre-prorenoguanylin is more homologous to pre-proguanylin than pre-prouroguanylin and a phen
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br Disclosure summary br Acknowledgments br Introduction Sym
2022-09-08
Disclosure summary Acknowledgments Introduction Symbionts are live microorganisms that seem to promote host defense systems and regulate intestinal homeostasis, preventing gut infectious and inflammatory diseases (Fuller, 1989, Sartor, 2004). Numerous studies have shown the beneficial effec
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We have previously established the pharmacokinetic profile
2022-09-08
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 V5 Epitope and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compoun
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Fmoc-Ser-OH Currently ursodeoxycholic acid UDCA is the only
2022-09-08
Currently, ursodeoxycholic Fmoc-Ser-OH (UDCA) is the only recommended and widely used drug in the treatment of CFLD. However, the clinical efficacy of UDCA is controversial. The most recent Cochrane review only identified a small number of trials assessing the effectiveness of UDCA [92]. The author
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br Advanced Glycation Endproducts As glucose levels rise wit
2022-09-08
Advanced Glycation Endproducts As glucose levels rise within sensory neurons as a result of hyperglycemia, normal metabolic pathways become overwhelmed and excess glucose is shunted into other ancillary pathways that, under these conditions, become damaging. One consequence of hyperglycemia is th
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br Secretase modulators a loss of pharmacology A lack
2022-09-07
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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Formyl peptide receptors FPRs are
2022-09-07
Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on
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The canonical tumor suppressor p has also been implicated
2022-09-07
The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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ADAM has two alternative splicing forms a
2022-09-07
ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto
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In C elegans KDM A appears to be involved
2022-09-07
In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene
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