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In summary we discovered azaindole
2022-04-18
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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The effect of GCK NES mutations on
2022-04-18
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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cAMP is a key secondary messenger which transduces extracell
2022-04-18
cAMP is a key secondary messenger which transduces extracellular signals at glucagon receptors to intracellular effector molecules. cAMP-protein kinase A (PKA) pathway increases the gene expression of enzymes including phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6-phosphatase (G6Pase) whic
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The vast majority of clinical studies have
2022-04-18
The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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Ghrelin is a brain gut peptide
2022-04-18
Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing
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br Methods br Results br Discussion In this series of
2022-04-18
Methods Results Discussion In this series of studies we hypothesized that FHH-GHSRm1/Mcwi rats would, relative to their WT counterparts, exhibit a metabolic and behavioral phenotype reminiscent of GHSR−/− mice. Through the use of the GHSR−/− mouse, a great deal about the role of ghrelin sig
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Introduction Parkinson s Disease PD is a neurodegenerative d
2022-04-18
Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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GOAT belongs to the super family of membrane bound
2022-04-18
GOAT belongs to the super family of membrane-bound O-acyltransferases (MBOATs). It is encoded by the gene MBOAT4 in human. The protein GOAT is highly conserved from zebrafish to human (Yanagi et al., 2018). GOAT is ubiquitously expressed with abundant expression in the stomach and intestine (Sakata
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br Materials and methods br
2022-04-18
Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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It must be noted that while the accumulated
2022-04-18
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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Introduction br Alzheimer pathology A and Tau Amyloid protei
2022-04-18
Introduction Alzheimer pathology: Aβ and Tau Amyloid β protein (Aβ) plays an important role in AD pathogenesis. At the molecular level, senile amyloid plaques and neurofibrillary tangles (NFT) are two neuropathological hallmarks of AD [1]. Mutations in genes encoding amyloid precursor protein (A
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br Results and discussion br
2022-04-18
Results and discussion Conclusion In normal and curd coconuts, full-length cDNA and parental genomic DNA sequences encoding endosperm specific AGal were sequenced and characterized. At least, three mutation colorimetric assay synthesis were identified in CnAGal gene. In vitro expression in K.
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br Summary br Conflict of interest br Acknowledgments
2022-04-18
Summary Conflict of interest Acknowledgments This study was supported by Grant No. 2014/13/B/NZ7/02277 from the National Science Centre, Poland. Introduction Progesterone (P) is an anticonvulsant hormone (Backstrom et al., 1984, Herzog, 1995, Herzog, 1999, Frye et al., 2000, Reddy, 2002
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In stark contrast to this study Zhang and colleagues
2022-04-18
In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC Lsodren treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment with the genotoxic
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Cy5 NHS ester (non-sulfonated) sale Compared to a large data
2022-04-18
Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi
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