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The usefulness of GIP R antagonism for the treatment
2022-09-01

The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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Nano biocatalyst prepared by assembling an
2022-09-01

Nano-biocatalyst, prepared by assembling an enzyme on nanomaterial (NM) carriers is an emerging innovation in the field of nanobiotechnology. Some of the advantages of using NM as supports in Bufalin to conventional porous supports are effective enzyme loading due to large surface area with reduced
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Next we studied the effects of the compounds PA Glu
2022-09-01

Next, we studied the effects of the compounds PA-Glu, PA-hSuc, and PA-hPim on the IGly of rat hippocampal neurons. As in the experiments with IGABA, IGly was affected by steroids with a pregnane skeleton, but not those with an androstane skeleton. At the same time, androstane steroids were shown to
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The overall very satisfactory potency profile
2022-09-01

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Carbenicillin core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly
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In contrast with the above
2022-09-01

In cp-690550 mg with the above results, in our GC model system, FPR1-, but not FPR2-knockout, enhanced tumour formation. However, it should be noted that the prominent role of mFPR2 with respect to mFPR1 in the mouse colon might be due to the significantly higher expression of mFPR2 than mFPR1 in th
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Recent research has focused on identifying key
2022-09-01

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty Cyclopamine receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it contributes to GLP
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Glucose metabolic pathways are well
2022-09-01

Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the PF-04691502 to respond to physiological changes [1]. Ovadi and Srere have suggested that a new
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lfm br Results br Discussion Previous
2022-09-01

Results Discussion Previous studies have shown that all the components of ET system are expressed by various neuronal and non-neuronal structures throughout the CNS (McCumber et al., 1990; Giaid et al., 1991). In effect, endothelin-converting enzyme activity, mRNA, ET-1 and ET-3 immunoreactivi
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br Discussion Our results showed that the
2022-08-31

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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Platycodon grandiflorum is a member
2022-08-31

Platycodon grandiflorum is a member of the genus Platycodon and is commonly known as balloon flower. In East Asia, P. grandiflorum is used for the treatment of asthma, coughs, inflammatory diseases, pulmonary tuberculosis, and diabetes (Takagi and Lee, 1972). Furthermore, recent studies have reporte
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The role of the cyclic AMP regulated exchange factor Epac
2022-08-31

The role of the cyclic AMP regulated exchange factor Epac1 is emerging in cancer (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). Interestingly, in cancer cell migration, activation of Epac1 can be linked to activation of Rac. As s
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br Mutagenesis and Receptor Modeling Studies br
2022-08-31

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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So far GnRH receptors have
2022-08-30

So far, GnRH receptors have been detected in the human ovary, but their physiological importance is still unclear (). In particular, GnRH receptors as well as GnRH types I and II have been localized in the granulosa Betaine of pre-ovulatory follicles, but not of follicles from the primordial to the
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Through the analysis of various synthetic
2022-08-29

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic 2825 australia motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discoveri
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Until recently the mechanism of how GSMs shifted secretase
2022-08-29

Until recently the mechanism of how GSMs shifted γ-secretase cleavage was poorly understood. Today, building on the sequential cleavage model developed by Ihara and colleagues [14], there is evidence that GSMs act as processivity enhancers, and iGSMs as inhibitors of processivity [120]. At least for
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