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For some agonists these stable GPR responses
2021-11-19
For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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For molecules with potential for therapeutic use
2021-11-18
For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low
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Here we examined whether complete
2021-11-18
Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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Human GS is a multi subunit complex consisting
2021-11-18
Human GS is a multi-subunit complex consisting of four components: presenilin 1 (PS1), presenilin enhancer 2 (PEN-2), anterior pharynx-defective 1A (APH-1A) and nicastrin (NCT) (Fig. 1a) [5,6]. PS1 comprise nine transmembrane helices (TM 1–9) and contains the catalytic aspartate residues in its TM6
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br Acknowledgments The research leading to these results was
2021-11-18
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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Aldicarb More recently Serna Marquez and
2021-11-18
More recently, Serna-Marquez and colleagues investigated LA-induced migration and invasion of MDA-MB-231 breast cancer cells. In this study, LA was shown to induce AKT-2 phosphorylation and cell invasion and migration in MDA cells. LA-induced cell migration was inhibited by siRNA that selectively ta
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While there have been a
2021-11-18
While there have been a variety of recent reviews on the signaling and physiological effects of FFA4, particularly towards its anti-inflammatory effects, the goal of this research update is to present the most recent details on the role of FFA4 in human cancers. The known contributions of FFA4 towar
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Type II diabetes is characterized by an inability
2021-11-18
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty ARRY-614 synthesis receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors and
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Several observations about structure activity relationships
2021-11-18
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic (E)-2-Decenoic acid class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ethe
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VDAC interacts with hexokinase and
2021-11-18
VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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It should be noted that one of
2021-11-18
It should be noted that one of the two phenyl groups of 15 is found in the main western pocket and the second phenyl group occupies the western secondary pocket (Ser53, Leu54, and Leu213). The nitrogen of the amide bond is involved in a hydrogen bonding interaction with Asp140. The alcoholic functi
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One of the key epithelium derived factors required
2021-11-18
One of the key epithelium-derived factors required to maintain immune tolerance in the intestine is Indian Hedgehog (Ihh). Ihh is secreted exclusively by intestinal epithelial cells, and signals in a paracrine manner to the inhibitory receptor Patched1 (Ptch1) on fructose 1 6 bisphosphatase in the
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br Methods br Results br Discussion Peptide therapeutics
2021-11-18
Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succe
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br Conclusions Beta cell specific expression in human islets
2021-11-18
Conclusions Beta cell-specific expression in human islets of DGCR2, GBF1, GPR44 and SerpinB10 has not previously been described, although the proteins have partly been characterized in other contexts not related to beta Aminophylline or diabetes. DGCR2, GPR44 and SerpinB10 were negative in all o
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br Conclusion We conducted single marker association and
2021-11-17
Conclusion We conducted single-marker association and haplotype association analyses of genetic mutations in porcine SLA-DOB and CD4 genes with T-lymphocyte subsets, cytokines, and droperidol in pregnant Landrace sows and obtained the SNPs and insertion that significantly affected the immunity t
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