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br Conclusions br Conflicts of interest
2021-12-15
Conclusions Conflicts of interest Funding The research work was partially supported by National Science Center (Contract Grant Number: UMO-2015/19/B/NZ1/00332). Introduction Frusectose-1, 6-bisphosphatase (FBPase) has long been recognized as a potential therapeutic target for the treatm
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br What are the local
2021-12-15
What are the local exocytotic protein targets of PKC? A direct method for PKC to potentiate insulin release would be to phosphorylate and activate components of the exocytotic machinery. Bulk measurements show that potentiation occurs by enhancement of the calcium sensitivity of exocytosis [56],
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In the previous study concerning HO mediated inhibtion of
2021-12-15
In the previous study concerning HO-1-mediated inhibtion of HCV replication, the mechanism underlying IFN-α/β indcuction by HO-1 involved in HO-1-catalyzed heme metabolic product, biliverdin (Zhu et al., 2010; Lehmann et al., 2010). However, in the present study SnPP, an inhibitor of HO-1 enzymatic
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In order to study the
2021-12-15
In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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ubiquinone coq10 br Conclusion br Disclosure of interest br
2021-12-15
Conclusion Disclosure of interest Acknowledgement Introduction Vitamin B6 has long been recognized as a cofactor for many enzymes, especially those involved in amino ubiquinone coq10 metabolism. Apart from its role as coenzyme, recent studies are unveiling a new role of vitamin B6 as a
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Z-WEHD-FMK In summary we have designed and optimized a new
2021-12-15
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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Migratory properties of Treg are
2021-12-15
Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing Acitretin australia into the inflamed tissue (in this case pancreatic islets). CXCR3 responds
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We also explored various nitrogen substituents
2021-12-15
We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, effl
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br Conflicts of interest br Funding This work was
2021-12-15
Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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br Introduction Major depressive disorder MDD is a disease w
2021-12-15
Introduction Major depressive disorder (MDD) is a disease with poorly recognized etiology. Currently used antidepressant drugs, which mainly affect synaptic neurotransmitter levels, show full clinical efficacy in only one third of patients (Rush, 2007). Thus it is now generally accepted that the
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Herein in consider of the high similarity
2021-12-15
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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The in vivo biological activity of the four novel analogues
2021-12-15
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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The usefulness of GIP R antagonism for the treatment
2021-12-15
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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pp2 Psoriasis is an inflammatory skin disease characterized
2021-12-15
Psoriasis is an inflammatory skin disease characterized by epidermal hyperplasia; micro-abscesses; neo-angiogenesis; a proinflammatory cytokine environment involving alterations of IL-17A, IL-23, and TNF-α; and activation of and infiltration by macrophages, mast cells, neutrophils, CD11c+ dendritic
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br Acknowledgements We apologize to our
2021-12-15
Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri
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