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In conclusion this is the
2022-06-05
In conclusion, this is the first description of a GPR81 agonist with an ability to exert in vivo efficacy without causing flushing. These results demonstrate that GPR81 small-molecule agonists may be effective for treating dyslipidemia. In addition, targeting GPR81 could prevent the unwanted side ef
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br Conflict of Interest Both GM and
2022-06-05
Conflict of Interest Both GM and BDH are shareholders in Caldan Therapeutics, a company exploring potential novel treatments for type 2 diabetes. Acknowledgments Work described herein was supported by Biotechnology and Biological Sciences Research Council [grant BB/K019864/1)] (to GM) and [gr
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TASIN-1 australia Considering the fact that OCL induced depl
2022-06-05
Considering the fact that OCL induced depletion of T TASIN-1 australia in non-stimulated cultures, the only possible explanation of this effect is the elevated mortality of these cells. It was found that OCL at the higher concentration induced the apoptosis of CD4+ and CD8+ T cells. These results s
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br Significant efforts are currently focused on
2022-06-05
Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) TAME hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-containing synapses, b
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A major hurdle in purifying a membrane
2022-06-05
A major hurdle in purifying a membrane protein is finding a detergent that can preserve the protein, after releasing it from a given membrane, in a stable and non-aggregated state during purification steps [18,50]. The ability of various detergents used to solubilize and purify membrane proteins has
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Both anxiety like behavior and
2022-06-05
Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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AG-120 A number of GCK activators for treating T
2022-06-05
A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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While ghrelin s role in addictive behaviors has been most
2022-06-05
While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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The highest metabolic stability observed
2022-06-05
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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Another TKI used in cancer therapy is
2022-06-02
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 RESULTS br DISCUSSION In this study we found impaired
2022-06-02
RESULTS DISCUSSION In this study, we found impaired apoptosis in the peripheral blood of RA patients when compared with peripheral blood from normal controls. Our previous studies have shown that the number of CD4 + T 2-Arachidonoyl Glycerol increased while regulatory T (Treg) cells diminished
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Our results are consistent with
2022-06-02
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral Y 134 as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts. A reduced num
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Dysregulation of the HPA axis resulting
2022-06-02
Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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Two classes of histones demethylases have
2022-06-02
Two classes of histones demethylases have thus far been identified: the Jumonji C (JmjC) domain-containing proteins and the amine oxidase domain (AOD)-containing proteins. They have distinct enzymatic mechanisms and substrate specificity. The JmjC domain is conserved through evolution and belongs to
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WAY-600 Metal organic frameworks MOFs have emerged over the
2022-06-02
Metal–organic frameworks (MOFs) have emerged over the past two decades with the potentials to act as promising materials in gas storage, chemical separation, catalyst, magnetism, sensing, and drug delivery etc (Du et al., 2013, Zhou and Kitagawa, 2014). Additionally, the secondary interactions, such
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