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br Materials and methods br Results br Discussion
2021-11-20
Materials and methods Results Discussion CRC and PC occupy a good share in cancer-related deaths worldwide. CRC is a common gastrointestinal malignancy with a growing incidence whereas PC is one of the most dreadful malignancies with extremely poor survival rates. Though over the past decad
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br Conflict of interest br
2021-11-20
Conflict of interest Acknowledgements A Class of Unconventional, Dimerization-Activated GTPases GTP-binding proteins, or GTPases, are a superfamily of proteins that regulate numerous cellular pathways 1, 2, 3, 4. Pioneering work on the extended Ras subfamily of GTPases, exemplified by Ras,
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In addition to understanding the GEF GAP cycle
2021-11-20
In addition to understanding the GEF-GAP cycle regulating Rho-family GTPases, studies have continued to address the role of the Rho-GDIs, which binds to the geranylgeranyl tail to sequester Rho-family GTPases from interacting with lipid membranes, preventing their activation. Whilst it would be temp
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Urinary hydroxypyrene OHP is a widely used biological marker
2021-11-20
Urinary 1-hydroxypyrene (1-OHP) is a widely used biological marker of exposure to PAHs and indicator for internal dose of activated PAHs (Jongeneelen, 1987, Adonis et al., 2003). PAH metabolites may be excreted either as free or as conjugated compounds. When 1-OHP is measured after treating the urin
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Acute effects of FZ were not altered in GluR A
2021-11-20
Acute effects of FZ were not altered in GluR-A−/− mice, thus providing a solid basis for comparing the effects of repeated drug administration. In addition, GluR-A subunit deficiency did not affect the basal behavior of saline-treated animals, despite the GluR-A−/− mice having been described as hype
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br Acknowledgments The financial support from the
2021-11-20
Acknowledgments The financial support from the National Natural Science Foundation of China (Nos. 31460422 and 31060210), the Natural Science Foundation of Jiangxi Province, China (20171BAB204029 and 20143ACB20006), the Project of Science and Technology of Jiangxi Provincial Education Department,
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br Conclusion In conclusion SHP
2021-11-19
Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to
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Flufenamic acid In conclusion enhanced glucagon action of th
2021-11-19
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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The fibroblast growth factor receptor FGFRs including
2021-11-19
The fibroblast growth factor receptor (FGFRs), including four highly conserved proteins (FGFR1-4), are important membrane sensors for extracellular signals [4]. By binding to their ligands, FGFRs are activated and can trigger various downstream intracellular signaling cascades, which is required for
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Acquiring resistance to the FGFR inhibitor
2021-11-19
Acquiring resistance to the FGFR inhibitor may determine treatment outcomes in patients with GC dependent on FGFR2 amplification, and we investigated the mechanism of AZD4547 resistance in FGFR2-amplified GC cells. We established a FGFR2-amplified GC cell line resistant to the selective FGFR inhibit
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To date the underlying mechanism of ropivacaine in inducing
2021-11-19
To date, the underlying mechanism of ropivacaine in inducing neurotoxicity remains unclear. Cell death was intimately involved in local-anesthetic neurotoxicity [6,18]. Two classic signaling pathways triggered cell death: the extrinsic pathway and the intrinsic pathway [12]. Our study demonstrated t
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br Materials and methods br Results br Conclusions In
2021-11-19
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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In conclusion a series of new carboxamido aryl isoxazoles wa
2021-11-19
In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed
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Myelination by oligodendrocytes is required for saltatory
2021-11-19
Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro
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P Benzoxaborole substituted macrocyclic compounds based on I
2021-11-19
P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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