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Nifedipine Recently a G protein coupled receptor GPR a
2022-03-12
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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Migratory properties of Treg are extremely important for
2022-03-12
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 Protionamide into the inflamed tissue (in this case pancreatic islets). CXCR3 responds to CXC
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In summary we have developed an
2022-03-12
In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ
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It is well known that GPCR responsiveness
2022-03-12
It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling
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As a part of our continuing efforts
2022-03-12
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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ATP is essential for maintaining
2022-03-12
ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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Olanzapine has been reported to
2022-03-12
Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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As cardiovascular disease accounts for the majority of
2022-03-12
As cardiovascular disease accounts for the majority of deaths in subjects with T2D, it is imperative that we better characterize the cardiovascular risks and benefits of the various therapies we prescribe to these individuals to control their glycemia. Indeed, the potential to identify subsets of di
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We speculated modulation of redox
2022-03-12
We speculated modulation of redox balance in brain, by activation of GIP receptor pathway. QA is known to mediate production of ROS, lipid peroxidation by its interactions with Fe2+ and formation of QA-Fe2+ complex (Braidy et al., 2010, Rios and Santamaria, 1991, Stipek et al., 1997). QA induces NOS
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It must be noted that while
2022-03-12
It must be noted that while the accumulated evidence on molecular mechanisms has resulted in well-established experimental methods to externally act on single-cell characteristics and networks, safe and efficient external methods to modify multicellular states are still a matter of basic research. C
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br Author contributions br Transparency document br Acknowle
2022-03-12
Author contributions Transparency document Acknowledgments The financial contributions of the Marie-Curie Action: BIOCONTROL, contract number MCRTN – 33439, the Agence Nationale de la Recherche (projects membraneDNP 12-BSV5-0012, MemPepSyn 14-CE34-0001-01, InMembrane 15-CE11-0017-01 and the
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At the end of experiments rats were
2022-03-12
At the end of experiments rats were injected high dose of sodium pentobarbital (90mg/kg) and the rat’s head was cut and frozen in −20°C for 20min with the injecting tube in situ before section. The location of the tip of the injecting tube was verified and all the tips of the injecting tube were in
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Of note the intracellular egg compartment exhibiting SA gal
2022-03-12
Of note, the intracellular egg compartment exhibiting SA-β-gal activity also exhibits lipofuscin auto-fluorescence (Fig. 6B), and it is co-stained with the lipid-specific dye SBB (Supplemental Fig. 5). On the one hand, these findings reflect the fact that the pool of yolk protein contains lipoprotei
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br The Farnesoid X receptor FXR identification and
2022-03-12
The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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Michiel S van der Heijden had full access
2022-03-12
Michiel S. van der Heijden had full access to all DPP4 Activity Fluorometric Assay Kit data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira,
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