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Recent pharmacological and clinical studies suggested that e
2021-01-05
Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and
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The upregulation of PTGS and PTGS
2021-01-05
The upregulation of PTGS1 and PTGS2 in late gestation in mares could be linked to the high levels of estrogens produced by the fetoplacental unit. Estrogens are thought to be effective stimulators of prostaglandin production by potentially up regulating PTGS2 expression. Although a recent publicatio
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Initially the cause of hypoglycemia
2021-01-05
Initially, the cause of hypoglycemia was not apparent. There was no detectable lesion in the pancreas on plain computed tomography, and anti-insulin antibody was negative. Eight hours after hospital admission, his son discovered that the patient had accidentally taken glimepiride 3mg/day for 3 days.
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In the present study the expression of the
2021-01-05
In the present study, the atipamezole of the CYP2C11 gene and the levels of its protein and activity were decreased in rats with liver insufficiency and in rats after induced dysfunction of the serotonergic system during normal liver function. Moreover, serotonergic system dysfunction during liver
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To develop antagonists selective for the mouse EP receptor
2021-01-05
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic 8-pCPT-2-O-Me-cAMP-AM synthesis () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced t
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Collectively our results indicate that GSK A functions as
2021-01-04
Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fig
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Programmed cellular death or apoptosis is a process genetica
2021-01-04
Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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Further indirect evidence supporting an
2021-01-04
Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc
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In conclusion we have found that Egr can play an
2021-01-04
In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response TAME at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promoter. We speculat
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The kinase activity of DNA PKcs
2021-01-04
The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], Tetracaine HCl IV [62],
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For the SAR optimization of the right hand side
2021-01-04
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic bazedoxifene synthesis moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced
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In this study we further investigated
2021-01-04
In this study, we further investigated the involvement of CRF1 and CRF2 receptors of the dPAG in the regulation of panic-related responses. For this, we used two animal models that associate escape behavior with panic attacks: the elevated T maze and the electrical stimulation of the dPAG (for a ful
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br Experimental br Declaration of interest br Introduction
2021-01-04
Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR acpt australia library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was modif
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T helper Th cells play a central
2021-01-04
T helper (Th) Necrostatin 2 play a central role in activation of immune system against infectious agents through secretion of lymphokines or cytokines. African trypanosomes target the Th cells and alter their activation, possibly for their own survival and perpetuity (Namangala, 2011). Trypanosoma
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br Conclusion br Conflicts of interest br
2021-01-04
Conclusion Conflicts of interest Acknowledgements This study was financially supported by The Science and Engineering Research Board (SERB), Department of Science & Technology (DST), Government of India under the Fast Track Scheme for Young Scientist to Dr. V. Dhananjayan (No: SB/FT/LS-140/
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