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The combination of niacin with a selective PGD
2022-04-08

The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su
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No other lacZ mutant showed
2022-04-08

No other lacZ mutant showed a marked difference in mutation rate between fpg and fpg backgrounds (that is, rates were comparable between HS101 and CSH1191, HS102 and CSH1192, etc.). The number of reversion mutants was much higher in HS1194 than in any other fpg strain. The inclusion of the pTRC99a
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Receptors for glucagon Gcgr GLP Glp
2022-04-08

Receptors for glucagon (Gcgr), GLP-1 (Glp1r), and GLP-2 (Glp2r) are G-protein coupled receptors (GPCRs) belonging to class B-1 (secretin receptor-like) family of GPCRs (Harmar, 2001, Fredriksson et al., 2003). The mammalian Gcgr, Glp1r, and Glp2r genes, together with the Fmoc-Ser-OH for the receptor
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There is increasing evidence that Cxs in astrocytes may play
2022-04-07

There is increasing evidence that Cxs in astrocytes may play a role in several models of brain pathologies. Interestingly their roles are at the moment more considered through their hemichannel function (Bennett et al., 2012; Bosch and Kielian, 2014; Davidson et al., 2013; Orellana et al., 2016; Kim
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Introduction br Alzheimer pathology A and Tau
2022-04-07

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 FGF FGFR pathway as predictive factor Several
2022-04-07

FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9 m
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br Acknowledgments This study was supported
2022-04-07

Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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Species specificity of small molecular
2022-04-07

Species specificity of small molecular GPR40 agonists have been reported by Takeda scientist. In the binding pocket of TM5, a Leu186 in human GPR40/FFA1 is replaced with Phe in rat, resulting in dramatic inter-species GPR40 activity discrepancy in certain scaffolds of small molecular GPR40 agonists.
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Receptor interactions and binding mode of in hGPR
2022-04-07

Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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To further investigate if GPR was
2022-04-07

To further investigate if GPR40 was the functional target of these phenylpropiolic pten pathway analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GP
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Nystatin Several transgenic and knockout congenic mouse
2022-04-07

Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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We have presented evidence that only muscle FBPase is detect
2022-04-07

We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart SC 144 receptor expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our preliminary
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Sperm exocytosis or acrosome reaction AR is a regulated secr
2022-04-07

Sperm exocytosis or acrosome reaction (AR) is a regulated secretion with special characteristics essential for fertilization. The AR relies on the same highly conserved molecules that drive intracellular membrane fusion and exocytosis in all other opioid receptor (see [59] for a recent review). Two
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br Materials and methods br Results
2022-04-07

Materials and methods Results Discussion It has previously been reported that EZH2 plays a key role in the silencing of tumour suppressor genes through methylation of H3K27me3 in the promoter region of these genes in neuroblastoma [32], [40]. In this study, we show that EZH2 is aberrantly g
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More recently Vismodegib was administered in combination wit
2022-04-07

More recently, Vismodegib was administered in combination with Gemcitabine in a pilot clinical trial that enrolled 23 patients affected by metastatic pancreatic adenocarcinoma. This type of malignancy is the most frequent form of pancreas cancer and is ranked in fourth place for cancer mortality in
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