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The effect of GCK NES mutations on
2022-09-17

The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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AR-A014418 In an immunohistochemical analysis of gastric can
2022-09-17

In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial AR-A01441
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br Author contributions statement P N Y designed
2022-09-17

Author contributions statement P.N.Y. designed the study, analyzed the data and prepared the draft of the manuscript. C.S performed the experiments, analyzed the data and generated Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5, Fig. 6, Fig. 7, Fig. 8. A.K. and S.D. made Supplementary Figs. S1 and S2. D.
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To evaluate the role of increased FPPS expression in
2022-09-17

To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on Peramivir progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cells (A and B),
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br Ethics statements br Introduction Hepatocellular carcinom
2022-09-17

Ethics statements Introduction Hepatocellular carcinoma (HCC) is the fifth most common malignant tumor and the third leading cause of cancer-related mortality worldwide, with rapidly-increasing incidence in recent years [1,2]. Mounting evidence shows that viral hepatitis, toxin exposure, non-a
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br Drug design Over the
2022-09-17

Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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Parkinson s disease is another neurodegenerative disorder
2022-09-17

Parkinson's disease is another neurodegenerative disorder affecting H3Rs. The most common clinical symptoms of this disease are rigidity, bradykinesia, rest tremor, loss of postural reflexes, and gain impairment owing to progressive degeneration of the dopaminergic neurons in the nigro-striatal neur
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Several studies have indicated that PLD
2022-09-17

Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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However despite medicinal chemistry efforts lead to consider
2022-09-17

However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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Suz is required for methyltransferase activity silencing
2022-09-16

Suz12 is required for methyltransferase activity, silencing function, and PRC2 protein stabilization in somatic and human ESCs (Cao and Zhang, 2004, Pasini et al., 2004, Collinson et al., 2016). Our experiments indicate that, in addition to associating with the H3K27 demethylases KDM6A (UTX) (Wang e
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All experiments in this study were performed at pD for
2022-09-16

All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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Bupivacaine is one of the local
2022-09-16

Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root 4μ8C (DRG) neurons [5], [6], [7], [8]
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br Mutagenesis and Receptor Modeling Studies
2022-09-16

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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Alamethicin The GPR gene was included
2022-09-16

The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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Our last area of exploration was the piperidine core as
2022-09-16

Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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