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Two recently developed highly specific EZH enzymatic inhibit
2022-04-15

Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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br Methods br Results We
2022-04-15

Methods Results We have previously used ß-hex assays in HeLa RN 1734 receptor to study the role of lysosomal exocytosis on transition metal clearance and the effects of transition metals on lysosomal exocytosis [26], [29], [40]. ß-hex is a lysosomal enzyme, the delivery of which to the extrac
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Furthermore the higher expression levels
2022-04-14

Furthermore, the higher expression levels of DNMT1 seemed to be responsible for the elevated levels of methylation in the GSTP1 and TXNRD2 promoters in HMC. In the DNA methyltransferase family, the functions of DNMT1 and DNMT3, including 3a and 3b, were the most ubiquitously expressed in cells. DNMT
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Despite having potent activity and
2022-04-14

Despite having potent activity and good solubility, showed inhibitory activities against cytochrome P450 (CYP) 2C8, 2C9, and 2C19 with an IC value of less than 10 μM. In general, the specificity of the compound to the target should improve and the off-target risk such as CYP inhibitory activity sho
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The global spread and ever increasing incidence of metabolic
2022-04-14

The global spread and ever-increasing incidence of metabolic syndrome over the past few decades has not only categorized it as an ‘epidemic’ but has also dramatically increased the risk of cardiovascular diseases and diabetes. The increase in prevalence of diabetes in the United States alone has bee
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EGTA Next we designed substituents of the position Edge
2022-04-14

Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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Heparin and suramin are highly negatively
2022-04-14

Heparin and suramin are highly negatively charged molecules, and they are in this aspect, similar to DNA and likely to compete with DNA by binding to the protein cationic groups [17] (Fig. 1). The inhibitory effect of heparin and suramin on DNA and RNA binding proteins has been described [[18], [19]
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Although side effects as paresthesia due
2022-04-14

Although side effects as paresthesia due to the application of β-alanine are known, a study in 2006 pointed out that there are no clinical (biochemical or hematological) changes after a long-term supplementation with β-alanine. In 2015, the International Society of Sports Nutrition rejected any argu
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br Materials and methods br Results Analysis of the
2022-04-14

Materials and methods Results Analysis of the post-mortem human prefrontal cortex by western blotting indicated that GLAST expression was increased 1.6-fold in the extracts of alcoholic brains relative to controls (Fig. 1A and B). To resolve the distinct sub-pools of GLAST within our samples w
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Long non coding RNAs lncRNAs are mRNA like
2022-04-14

Long non-coding RNAs (lncRNAs) are mRNA-like transcripts of greater than 200 nucleotides (nt), with little or no protein-coding potential [13,14]. LncRNAs have been suggested to participate in transcription and post-transcription regulation as scaffolds, guides, decoys or repressors, activators, and
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br Methods br Acknowledgements The authors
2022-04-14

Methods Acknowledgements The authors thank the ZLS group members, particularly Li Li and Elijah Roberts, for many helpful discussions. They also wish to thank Nathan Baker for APBS assistance, Jan Jensen for help with PROPKA 2.0, Susan Martinis for experimental interpretations, and John Stone
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In conclusion enhanced glucagon action of
2022-04-14

In conclusion, enhanced glucagon action of the beta cell results in improved beta cell function after glucose stimulation, but simultaneously dissociated responses to both glucose-dependent and non-glucose secretagogues evolve. This shows that the glucagon receptor is complexly involved in beta cell
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Gastric inhibitory polypeptide a hormone belonging to the gl
2022-04-14

Gastric inhibitory polypeptide, a hormone belonging to the glucagon-secretin family of peptides, exhibits protection against the neurodegeneration and also stimulates neurogenesis in adult rats in a paracrine manner (Gault and Holscher, 2008, Nyberg et al., 2005, Usdin et al., 1993). The expression
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Gastric inhibitory polypeptide a hormone belonging to the gl
2022-04-14

Gastric inhibitory polypeptide, a hormone belonging to the glucagon-secretin family of peptides, exhibits protection against the neurodegeneration and also stimulates neurogenesis in adult rats in a paracrine manner (Gault and Holscher, 2008, Nyberg et al., 2005, Usdin et al., 1993). The expression
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br Genetic manipulation variation of the ghrelin
2022-04-14

Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors
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