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Glycine regulates several brain functions
2021-11-24
Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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br Endogenous lipids as SLC transporter modulators
2021-11-24
Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure [
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It is increasingly argued that the immunosuppressive effects
2021-11-24
It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit PRT 4165 of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with the idea that GC-mediated repressio
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Olanzapine has been reported to attenuate insulin secretion
2021-11-24
Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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Two excellent GSMs with clear pharmacological effect
2021-11-24
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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Recently a lot of synthetic FFA
2021-11-24
Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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Main Text FFAR GPR is a long chain
2021-11-24
Main Text FFAR1 (GPR40) is a long-chain fatty adenosine receptor (LCFA) receptor highly expressed and enriched in enteroendocrine cells, where it senses LCFAs generated from dietary triglycerides, and in pancreatic islet cells, where it acts as a powerful stimulator of insulin secretion. However, t
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br Introduction Atrial fibrillation is the most
2021-11-24
Introduction Atrial fibrillation is the most common cardiac arrhythmia (Benjamin et al., 1998). Pulmonary vein (PV) sleeves contain a mixture of working myocardium and potential arrhythmogenic pacemaker g protein coupled receptors behaving as an ectopic trigger of atrial fibrillation (Haissaguer
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We conclude that a combination of GD specific CAR
2021-11-24
We conclude that a combination of GD2-specific CAR T cell therapy with pharmacological EZH2 inhibition deserves investigation as a new therapeutic strategy in EwS and potentially other cancers with heterogeneous GD2 expression, including osteosarcoma, various soft tissue sarcomas, melanoma, lung can
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br The inhibitory effect of ATP B knockdown on lysosomal
2021-11-24
The inhibitory effect of ATP7B knockdown on lysosomal exocytosis is likely mediated by the resulting oxidative stress induced by Cu, as exposure to oxidative stress induced by tert-Butyl hydroperoxide (TBHP) inhibited β-hex exocytosis as well, indicating that oxidative stress inhibits lysosomal ex
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Mammals adapt to prolonged periods of food scarcity by relea
2021-11-24
Mammals adapt to prolonged periods of food scarcity by releasing FFAs from adipose tissue and transforming them into energy-rich ketone bodies that are used as fuel by brain, muscle, and other organs (Kersten, 2014, Grabacka et al., 2016). Ketogenesis occurs primarily in hepatocytes, but its rate is
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Long non coding RNAs lncRNAs are a class
2021-11-24
Long non-coding RNAs (lncRNAs) are a class of RNA transcripts which are over 200 nucleotides in length and not translated into proteins (Ponting et al., 2009). Recent studies showed that lncRNAs have been identified as crucial regulators of gene expression, chromatin remodeling, and cell cycle (Wahl
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HER genotype was determined in breast cancer tissue of breas
2021-11-24
HER2 genotype was determined in breast cancer tissue of 73 breast cancer patients. As previously reported, Ile655Val and Ala1170Pro genotypes measured in breast cancer tissues were available for 71 and 69 breast cancer patients, respectively. Briefly, 77.5% (55/71) of patients were homozygous for th
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One of the key epithelium
2021-11-24
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 Regorafenib synthesis in the mesen
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br Methods br Results br Discussion Peptide therapeutics
2021-11-23
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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