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Acute in vivo experiments were performed in normoglycemic SV
2021-09-23
Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding tubulin control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produced an
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LPC OMe LPC LPC and OMe
2021-09-23
LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated BIX 01294
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Introduction Cancer is known as a
2021-09-23
Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous ezh2 inhibitor synthesis have the ability to bypass the normal apoptosis mechan
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In the present study five Glu substituted analogues of
2021-09-23
In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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We are aware that the
2021-09-23
We are aware that the classical biochemical view is centered on the local concentrations of specific ion and molecules rather than on cell electric potentials. However, important downstream processes can be influenced by acting locally on these potentials because they regulate the conductance of the
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br Declarations of interest br Acknowledgements
2021-09-23
Declarations of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81673321, 21506099), the State Key Laboratory of Drug Research (SIMM1705KF-13), the Natural Science Foundation of Jiangsu Province (Grant No. BK20151541), and the Jiangsu Syne
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br Discussion and concluding remarks FPR is considered
2021-09-22
Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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The above inferences concluded that histidine is
2021-09-22
The above inferences concluded that histidine is enhancing the overall stability and rigidity of the protein which further might be restraining the protein during the transition from inactive to active state and vice-versa present in the SANT domain. Since the SANT domain binds with histone via elec
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br Conclusion The addition of cellulose to natural
2021-09-22
Conclusion The addition of gaba receptors to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H-bonds wh
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The current research also analyzed the association of this p
2021-09-22
The current research also analyzed the association of this polymorphism with HCV genotype 1-related hepatic steatosis by gender. Even though the allele and genotypes of this polymorphism an increased the risk of HCV-related hepatic steatosis, neither allele nor genotype frequency of this polymorphis
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Aclacinomycin A br Future perspectives sGC signaling is impo
2021-09-22
Future perspectives sGC signaling is important in the maintenance of multiple physiological functions. sGC is localized to cell membranes with both sGC Cys modifications and heme regulation identified as the crucial components in regulating sGC activity. Specifically, S-nitrosation of several com
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Racemic protein crystallography has been proven to be
2021-09-22
Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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Here we investigate the structural and biochemical propertie
2021-09-22
Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or raas inhibitors
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Decreasing GSK activity has therapeutic benefits in animal m
2021-09-22
Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic NS3694 injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregulating Aβ cleara
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Numerous stimuli lead to inactivation of GSK
2021-09-22
Numerous stimuli lead to inactivation of GSK-3, including Growth Factors such as EGF (Epidermal Growth Factor), PDGF (Platelet-Derived Growth Factor), BDNF (Brain-derived neurotrophic factor), IGF (Insulin-like growth factor) and insulin (Beaulieu et al., 2009, Chen and Russo-Neustadt, 2005, Cohen a
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