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br GSK The GSK family is highly conserved
2021-10-23
GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in hydrazone [1]
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Typically upon chronic agonist exposure
2021-10-23
Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have
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However even if immunological tests with the NQ peptide
2021-10-23
However, even if immunological tests with the NQ21 peptide are mostly positive [8], it doesn't mean that the structure of the NQ21 peptide is the same as that of the corresponding gp120 region characterized by a long alpha helix. Therefore, the aim of the current work was to check whether the NQ21 p
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br STAR Methods br Introduction Glycosylation is one of the
2021-10-23
STAR★Methods Introduction Glycosylation is one of the most prevalent post-translational modifications of proteins. It not only plays major roles in folding, transport and localization of proteins [1], but also regulates various biological processes such as cell growth, viral replication and im
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Transporters are important ta http www apexbt com media
2021-10-23
Transporters are important targets for devising new therapies, optimizing existing therapies, and helping understand the toxicities of certain drugs. Given the well-documented role of transporters in restricting the distribution of drugs, modulating the relevant transporters could enhance the permea
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br Experimental section br Results
2021-10-22
Experimental section Results and discussion Conclusion The evaluation of the inhibitory potential of these derivatives towards eight kinases showed that the brominated hybrids (3k) and (3l) are the most active against the PIM1 and CLK1 kinases. The methylation of the nitrogen Saikosaponin A
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Further SAR was explored with the imidazole
2021-10-22
Further SAR was explored with the imidazole series to achieve better enzyme inhibition activity (). In comparison to published earlier, replacing the amide with sulfonamide and reverse sulfonamide maintained the GSNOR inhibitory activity. It is clear that exchanging the phenyl ring (, and ) by t
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Methylpiperidino pyrazole br Concluding Remarks Given the in
2021-10-22
Concluding Remarks Given the increasing global incidence of metabolic disorders, new drugs that lower body weight and improve glucose tolerance are desperately needed. While we still have a long way to go, GPR55 might be an interesting target to explore, given its expression in numerous metabolic
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br Conclusions br Introduction G protein coupled receptors
2021-10-22
Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as
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br Signaling pathways activated by pulsatile GnRH In
2021-10-22
Signaling pathways activated by pulsatile GnRH In the pituitary, GnRH acts by binding to the G protein-coupled GnRHR on the cell surface of the gonadotrope, inducing interaction of the receptor with heterotrimeric G proteins and catalyzing GTP-GDP exchange on the G protein α subunit (Lambert, 20
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br Origin of the vertebrate hexokinase gene
2021-10-22
Origin of the vertebrate hexokinase gene family Multiple hexokinases have been found in vertebrates, plants and yeast (Wilson, 1995, Cárdenas et al., 1998). A hexokinase in both vertebrates and yeast has, unfortunately, been named glucokinase. The sharing of the name glucokinase has suggested to
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br Acknowledgements Research was funded by the Natural Scien
2021-10-21
Acknowledgements Research was funded by the Natural Sciences and Engineering Council of Canada (NSERC) (Grant #210290) SGF. The funding body played no role in the design or execution of the study. The authors declare no conflict of interest. Introduction HBO2 therapy is the use of 100% oxygen
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In summary two new flexible
2021-10-21
In summary, two new flexible amine-functionalized quinolinium derivatives with far-red region emitting were prepared. The shorter-chain fatty amine side chain in the scaffold of was found to be a more promising G-quadruplex DNA fluorescent probe, suggesting the amine side group plays an important ro
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The neurotransmitter histamine plays a key role in the sleep
2021-10-21
The neurotransmitter histamine plays a key role in the sleep-wake cycle and in learning and memory. Alterations in ML133 HCl histamine levels are closely connected with central nervous system dysfunction, and are thought to contribute to neurological disorders, including Alzheimer's disease and dep
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Tylophora atrofolliculata is a centuries
2021-10-21
Tylophora atrofolliculata is a centuries-used folk medicine for the treatment of rheumatism in China (Jiangsu New Medical College, 1977). One group of its bioactive components is phenanthroindolizidine alkaloids, which have been demonstrated as lead compounds of anti-tumor agents in our previous stu
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