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br Acknowledgements Research was funded by the Natural
2021-11-18
Acknowledgements Research was funded by the Natural Sciences and Engineering Council of Canada (NSERC) (Grant #210290) SGF. The funding body played no role in the design or execution of the study. The authors declare no conflict of interest. Introduction HBO2 therapy is the use of 100% oxygen
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br Results and discussion br
2021-11-18
Results and discussion Conclusion In the continued SAR study of our previous heterocycle scaffolds represented by SC75741 sale 2, we focused especially on improving their drug-like physicochemical properties directed by lipophilicity, LE and LLE. After explored several heterocyclic scaffolds,
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Another TKI used in cancer therapy is the Abl
2021-11-18
Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation [
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br Introduction The brain contains abundant fatty acids whic
2021-11-18
Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in d
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During the activation of the
2021-11-18
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium LY2606368 HCl on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit
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Histamine receptors were largely linked with allergic and in
2021-11-18
Histamine receptors were largely linked with allergic and inflammatory reactions before the recognition of the histamine H3R in 1983 that proved its function as auto- as well as heteroreceptor at pre- and postsynaptic membranes and demonstrated its intense regulating influence on release of numerous
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antioxidants br Conclusions In summary our results
2021-11-18
Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical antioxidants have a dual effect, and a decrease of the 5-HT2A
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br Conflict of interest br Introduction Endometriosis is def
2021-11-18
Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent
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Over the last years numerous studies gave
2021-11-18
Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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br Introduction The Ras superfamily of small GTPases is
2021-11-18
Introduction The Ras superfamily of small GTPases is composed of more than 150 protein members involved in a wide variety of biological processes, such as proliferation, differentiation, cytoskeletal organization, and protein trafficking [1]. The Ras superfamily proteins act as molecular switches
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br Concluding Remarks Given the increasing global incidence
2021-11-18
Concluding Remarks Given the increasing global incidence of metabolic disorders, new drugs that lower body weight and improve glucose tolerance are desperately needed. While we still have a long way to go, GPR55 might be an interesting target to explore, given its expression in numerous metabolic
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AKR D is very highly expressed
2021-11-17
AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv
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Interestingly GAL has also been shown to be
2021-11-17
Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion
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Neovascularization upon IMQ treatment was observed to differ
2021-11-17
Neovascularization upon IMQ treatment was observed to different degrees in WT and GAL3-KO mice, whereas the increase in vascular endothelial growth factor mRNA levels was genotype independent. Because we observed lower levels of the cytokines IL-17A, IL-22, IL-23, and TNF-α in IMQ-treated skin of GA
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FXR agonists represent an attractive class of
2021-11-17
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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