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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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Despite the central role of mitochondria in
2022-08-29
Despite the central role of mitochondria in oxidative metabolism, it remains unclear whether mitochondria play a central role in ferroptosis. Supporting this possibility, ferroptosis is associated with dramatic morphological changes of mitochondria, including mitochondrial fragmentation and cristae
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There have already been many reports on the AFS
2022-08-29
There have already been many reports on the AFS gene (Beuning et al., 2010, Green et al., 2007, Li et al., 2006, Pechous and Whitaker, 2004, Pechous et al., 2005, Yuan et al., 2007, Yuan et al., 2010) and HMGR gene (Pechous and Whitaker, 2002, Rupasinghe et al., 2001). The recent advances concerning
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br Materials and methods br Results
2022-08-27
Materials and methods Results Discussion EZH2 is a subunit of the polycomb repressive complex, which trimethylates lysine 27 on histone 3, a repressive marker for gene expression. EZH2 is important for cancer cell proliferation, migration, and invasion, all of which are associated with canc
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