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In addition researchers studying GPR agonists favor the
2022-04-06

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it N1-Methylpseudouridine is unclear why Sanofi-Aventis chose to terminate collaboration wi
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read what he said Because of its excellent GPR potency good
2022-04-06

Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, read what he said was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive p
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br Author contributions br Acknowledgements The work was fin
2022-04-06

Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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Heparin and suramin are highly negatively charged molecules
2022-04-06

Heparin and suramin are highly negatively charged molecules, and they are in this aspect, similar to DNA and likely to compete with DNA by binding to the protein cationic groups [17] (Fig. 1). The inhibitory effect of heparin and suramin on DNA and RNA binding proteins has been described [[18], [19]
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After brain injury adenosine levels
2022-04-06

After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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br Characterization and regional localization
2022-04-06

Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr
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A key limiting factor in the
2022-04-06

A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of eg5 of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This necessitates
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In order to consolidate our genetic funding we performed
2022-04-06

In order to consolidate our genetic funding, we performed several in silico analysis regarding the p.R85W mutation. The high conservation of R85 residue in all species suggests that it has an important role in glucokinase function. Pathogenic effect of the p.R85W is supported by in silico prediction
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br Results br Discussion Our cardiomyocyte specific GR knock
2022-04-06

Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR Latrunculin B receptor mouse model using GR-floxed
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Introduction Parkinson s Disease PD
2022-04-06

Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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br Some general considerations on anterior pituitary cell
2022-04-06

Some general considerations on anterior pituitary cell type, models, sex and drugs Historically, real-time analysis of native endocrine anterior pituitary cell excitability has been somewhat limited and thus much of the pioneering work on anterior pituitary cell excitability and stimulus-secretio
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The observed CORT induced increase in Cx
2022-04-06

The observed CORT-induced increase in Cx43 phosphorylation at S368 may also contribute to GJIC disruption. Gap junction channel permeability is modulated through connexin phosphorylation (Moreno and Lau, 2007). Specifically, the phosphorylation of Cx43 on S368 has been previously shown to decrease i
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The present data suggest that the decrease of liver BAs
2022-04-06

The present data suggest that the decrease of liver BAs was mainly due to the decrease of hepatic BAs synthesis because the BA synthetic enzymes Cyp7a1, Cyp7b1 and Cyp8b1 were markedly reduced. The increase may also be due to the increase of hepatic BAs efflux, because the liver BA efflux transporte
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The receptor binding assay used in
2022-04-06

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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Pattern recognition receptors key elements in
2022-04-06

Pattern recognition receptors - key elements in the innate immune response Every day, human beings are exposed to a broad range of microbes and foreign substances. Most of them are entirely harmless, however, some are pathogenic and have the potential to cause severe harm. The distinction between “
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