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cisapride synthesis br Mechanisms of Resistance As with othe
2022-01-06
Mechanisms of Resistance As with other cancer treatments in development, resistance is a concern with HHIs. Most observations regarding HHI resistance originate from patients with BCC [78]. In the clinic, resistance to vismodegib and sonidegib were observed when used to treat advanced BCC [78], [
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The global spread and ever increasing incidence of metabolic
2022-01-05
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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br Materials and methods br Results br Discussion
2022-01-05
Materials and methods Results Discussion DNA repair pathways have evolved for a long time to act independently of one another. However, over the past decade several overlaps and crosstalks between these pathways were identified, showing that the DNA repair system is more complex than previo
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br Regulation of Glu transporters The pivotal
2022-01-05
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino ACY-241 calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcriptio
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A number of anti diabetic drugs are available that
2022-01-05
A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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The effect of GCK NES
2022-01-05
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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Exposure of human and animals to MPTP can
2022-01-05
Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA
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Communication through GJ channels is regulated at different
2022-01-05
Communication through GJ channels is regulated at different levels and includes GJ plaque internalization into a single cell. Those vesicles contain the membrane of both cells and th assembled Cx43. The C-terminal domain of Cx43 interacts with different peptides and proteins. However, the internaliz
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Although NCT undergoes complex glycosylation processing for
2022-01-05
Although NCT undergoes complex glycosylation processing for maturation through trafficking from endoplasmic reticulum to Golgi or additional compartments, the effect of NCT glycosylation on γ-secretase activity and substrate specificity is still unknown. The present study focused on glycosylation st
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In conclusion a novel series of
2022-01-05
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen apoptosis inducer had a remarkable effect on the GPR40 agonistic ac
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Over decades a deeper understanding of terpene synthases has
2022-01-05
Over decades, a deeper understanding of terpene synthases has also permitted enzyme engineering for unnatural substrate acceptance. Novel terpenoids have been successfully synthesized from substrate analogues as by-products from mechanistic investigation (Faraldos et al., 2012; Miller, Yu, & Alleman
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Potential platelet related mechanisms that might explain
2022-01-05
Potential platelet-related mechanisms that might explain an augmented risk of MI in dabigatran treated patients have been investigated: Enhanced platelet reactivity is known to be associated with the risk of MI (Mangiacapra et al., 2018) and catalytically active thrombin is a potent stimulus to indu
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PKC does not however directly stimulate secretion by
2022-01-05
PKC does not, however, directly stimulate secretion by initiating calcium influx into the cell [51]. Work from multiple groups measuring calcium currents has shown that PMA alone or coupled with glucose does not modulate intracellular calcium influx [34], [51], [52], [53]. Instead of contributing to
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br Acknowledgements br Insulin is a vital peptide
2022-01-05
Acknowledgements Insulin is a vital peptide hormone with the exclusive capacity to regulate the blood glucose that entirely is secreting from pancreatic β cells (Kasai et al., 2014). The human insulin comprises 51 amino SBI-0206965 residues, with a molecular mass of 5.808 kDa. INS, responsible
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Following the discovery of diketo compounds S and L as
2022-01-05
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent AG-120 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioassa
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