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As comparators compounds and were made
2021-11-18
As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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The physiological and pharmacological roles of
2021-11-18
The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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In normal tissues the expression patterns of
2021-11-18
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet JNJ-1661010 and intestinal tract [7], [20]. It is considered that the distribution of the GPR
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GLP is an intestinal peptide hormone that
2021-11-18
GLP-1 is an intestinal peptide hormone that is released by the gut following ingestion of food, particularly NHS-12-Biotin synthesis and fats. Following its release, GLP-1 stimulates pancreatic β-cells to secrete insulin (Hirasawa et al., 2005, Covington et al., 2006). Originally, GLP-1 acted in a
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br Materials and methods br Results br Discussion br Disclos
2021-11-17
Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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SGCs tightly ensheath the soma of DRG
2021-11-17
SGCs tightly ensheath the soma of DRG neurons (Costa and Moreira, 2015, Hanani, 2005, Takeda et al., 2009). Intimate associations between SGCs and neurons facilitate bidirectional regulation of SGC function and neuronal excitability. After nerve injury, neuronal hyperexcitability can result in SGC a
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Studies regarding secretase nowadays aim
2021-11-17
Studies regarding γ-secretase nowadays aim at elucidating how APP is recognized and recruited. It has been suggested based on coarse-grained molecular simulation that the recognition and recruitment of substrate can occur on an extended surface covering PS1's TM2/6/9 domains and PAL motif [15]. Tran
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br Acknowledgments The research leading to these
2021-11-17
Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/
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The intestinal epithelium is the first line of defense again
2021-11-17
The intestinal epithelium is the first line of defense against pathogens and noxious agents and exerts a range of physiological activities, including digestion and CCT137690 of nutrients. The intestinal wall consists of a series of finger shaped protrusions called villi and invaginations known as c
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SH-4-54 australia In this study we have investigated the exp
2021-11-17
In this study, we have investigated the expression of FXR and TGR5 in CCA tissues in two independent cohorts of patients and determined their association with tumor clinicopathological parameters. The expression of both BA receptors was also evaluated in CCA human cells and normal human cholangiocyt
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Fpr which belongs the family of
2021-11-17
Fpr1, which belongs the family of the formyl peptide receptors with FPRL1 and FPRL2, is the principal receptor for formylated peptides which prototype is the tri-peptide fMLF. Fpr1 is highly expressed on neutrophils and macrophages [6,30], promotes their migration into the mucosa and lumen in respon
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The canonical tumor suppressor p has also been
2021-11-17
The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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The anti platelet functions of ZGR were confirmed by the
2021-11-17
The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagati
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br Application of TIRFM to visualizing exocytosis
2021-11-17
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin 98 2 (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant mice, or s
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Dithiodipyridine also known as aldrithiol is a known zinc ej
2021-11-17
2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency Pregnenolone Carbonitrile type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamin
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