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One possible pitfall of using EPAC activators in the
2021-06-11

One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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LDC1267 br Methods Ventricular cardiomyocytes from adult mal
2021-06-11

Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10μ
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Although the mechanisms underlying the EP
2021-06-11

Although the mechanisms underlying the EP4-mediated increase in the frequency of mEPSCs via PGE2 remain unclear, mechanisms similar to those driven by EP2 may be involved because activation of both these receptor subtypes increases the intracellular concentration of cAMP (Nishigaki et al., 1995, Sug
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br Acknowledgements This research was supported by Slovenian
2021-06-11

Acknowledgements This research was supported by Slovenian Research Agency (ARRS). We thank prof. R. Marinšek Logar for helpful advice, Dr. T. Kranjc for help with data management, N. Vrhovnik and G. Lavrič for technical help with preliminary growth experiments and dr. J. Burkeljca for help with g
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br Introduction Our understanding of how ligands interact wi
2021-06-11

Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc
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Overall the evidence and the results from in vivo
2021-06-11

Overall, the evidence and the results from in vivo studies clearly indicate that cyclosporine biotransformation can be induced by dasatinib co-administration through induction of CYP3A expression. However, further studies are needed to explore the role of P-gp modulation in DDIs. Conclusion In v
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CYP A is involved in the
2021-06-10

CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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The on target in vitro pharmacology of was then further
2021-06-10

The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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KB-R7943 mesylate receptor In we studied normal rational var
2021-06-10

In [1] we studied normal, rational -varieties X of complexity one, where the latter means that X comes with an effective torus action such that holds. We showed that for affine X with and at most log terminal singularities, the iteration of Cox rings is possible. In the present article, we charac
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fgf receptor inhibitor VHb expression in recombinant E coli
2021-06-10

VHb expression in recombinant E. coli expressing P4H improved Hyp production, presumably by enhancing oxygen transfer. VHb expression contributed to improving growth and extending the period of exponential growth in both shaker flask culture and bioreactor fermentation. A similar phenomenon was als
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As mentioned above disruption of Tgif in mice is
2021-06-10

As mentioned above, disruption of Tgif1 in mice is associated with dyslipidemia, and here we investigate the effects of overexpression of TGIF1 on expression of the Npc1l1 gene and markers of intestinal cholesterol absorption. Materials and methods Results Discussion In this study, we soug
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This approach is similar to that
2021-06-10

This approach is similar to that suggested by the previous edition of the GL [6]. Not surprisingly, the questions to be answered are the same (i.e., was the event TLOC? In cases of TLOC, is this (R)-PFI 2 hydrochloride mg of syncopal or non-syncopal origin? In cases of suspected syncope, is there a
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The preceding results show no
2021-06-10

The preceding results show no association between the EP1 gene polymorphisms and suicide completers in the Japanese population. Impulsive aggression is one of the most important risk factors for suicide especially in the younger generation (Brent et al., 2002, Melhem et al., 2007). EP1 knockout mice
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br Activatable MRI probes MRI is commonly used
2021-06-10

Activatable MRI probes MRI is commonly used in clinics around the world and has the advantages of outstanding tissue-penetration depth and extremely high spatial resolution for in vivo imaging [33]. MRI has relatively poor sensitivity and usually requires 6206 agents to enhance the imaging contr
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The Acat gene was identified by functional complementation o
2021-06-10

The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, abiraterone acetate 1 and 7, with each site containing a distinct promoter: chromosome 1 conta
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