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The effect of GCK NES mutations on
2021-12-24

The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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The ER EK polymorphism is located in the
2021-12-24

The ER22/23EK polymorphism is located in the transactivation domain of the GR gene. A single nucleotide polymorphisms (SNPs) has been identified in both of the two adjacent codons (22 and 23). These SNPs are fully linked and are associated with relative GC resistance[32], [44]. Although no associati
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As cardiovascular disease accounts for the majority of death
2021-12-24

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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Recently multiple receptor agonists have been developed to t
2021-12-24

Recently, multiple receptor agonists have been developed to treat type II diabetes (Finan et al., 2013, Finan et al., 2015). We have tested novel dual GLP-1/GIP receptor agonists that showed good neuroprotective effects that are superior to single GLP-1 analogues (Cao et al., 2016, Jalewa et al., 20
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Exposure of human and animals to
2021-12-24

Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA n
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br Introduction Ghrelin is a amino acid
2021-12-24

Introduction Ghrelin is a 28-amino TASIN-1 peptide mainly produced in the stomach and small intestines with the kidneys, placenta, and pancreas contributing to miniscule amounts of circuiting ghrelin [1]. Ghrelin exists in circulation in two major forms: acyl ghrelin (AG) and desacyl ghrelin (DA
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br Activators Many compounds are known to influence the
2021-12-24

Activators Many compounds are known to influence the activity of Ca2+-activated K+ channels, and since hIK1 was cloned more insight has been gained on compounds that have the capacity to increase channel activity. Activation by divalent metal cations has been investigated, with Ca2+, Pb2+, Cd2+,
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br Introduction Connexins are transmembrane proteins
2021-12-24

Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent Tenovin-6 via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nutrients to the extracellula
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Vancomycin hydrochloride Together our data are consistent wi
2021-12-23

Together, our data are consistent with the idea that the antidepressant-like effect of a low dose of galanin administration in the DRN would be mediated by the activation of local GAL2. To support this hypothesis, we set an additional experiment to evaluate whether the antidepressant-like effect of
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br Results and discussion The synthesis of
2021-12-23

Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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Compounds were tested for GPR activity in a functional
2021-12-23

Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO I-BET151 transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity relat
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Darifenacin HBr Autophagy plays a multifaceted role in regul
2021-12-23

Autophagy plays a multifaceted role in regulating both the quality and quantity of protein (e.g., protein half-life and activity) and organelles (e.g., mitochondrial number and function), thus determining cell fate [15]. The induction of autophagy has been generally considered a programmed cell surv
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br Materials and methods br Results The immunoblot
2021-12-23

Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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In the next set of experiments we sought to
2021-12-23

In the next set of experiments, we sought to determine the source of lysosomal p-Chlorophenylalanine inhibition by oxidative stress. Lysosomal exocytosis probably involves multiple steps including vesicle positioning, delivery, docking and fusion. The previous evidence and data in Fig. 1C,D show th
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br Expression and Purification of LSD Proteins
2021-12-23

Expression and Purification of LSD1 Proteins In Vitro Enzymatic Assays Analysis of LSD1 Demethylase Activity Acknowledgments Conflict of Interest Statement: Y.S. is a cofounder of Constellation Pharmaceuticals, Inc. and is a member of its scientific advisory board. Y.S. is also a consu
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