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Receptor interactions and binding mode of in hGPR
2022-02-18
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulati
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Several small molecules such as erastin and
2022-02-18
Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer gpr120 agonist [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-depende
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br Role of funding source br Conflict
2022-02-18
Role of funding source Conflict of interest Acknowledgements We thank F. Blaskovits and P. Kesner for technical assistance. This project was supported by operating grants from the Canadian Institutes of Health Research (CIHR) to X. Zhang (MOP123249) and the National Natural Science Foundati
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Development of few more dihydroxy pyrimidine and N
2022-02-18
Development of few more dihydroxy-pyrimidine and N-methylpyrimidone analogues as HIV-integrase inhibitors was attempted involving substitution of variety of five- and six-membered rings via the introduction of a simple methyl substituent in the α-position of the C-2 side chains in order to improve p
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Despite these multiple mechanisms of
2022-02-18
Despite these multiple mechanisms of viral persistence, one patient has been reportedly cured from HIV-1 infection . Timothy Brown, also known as the 'Berlin patient', was diagnosed with HIV-1 infection in 1995. After controlling viremia for several years via cART, he was diagnosed with acute myeloi
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In NAFLD models the first
2022-02-18
In NAFLD models, the “first hit” is liver fat accumulation, which causes insulin resistance, whereas the interplay of inflammatory cytokines, which causes inflammation, acts as the representative “second hit” [9]. However, recently, the “multiple hit” hypothesis has taken into consideration that mul
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Long non coding RNAs lncRNAs are a class of RNA
2022-02-18
Long non-coding RNAs (lncRNAs) are a class of RNA transcripts which are over 200 nucleotides in length and not translated into proteins (Ponting et al., 2009). Recent studies showed that lncRNAs have been identified as crucial regulators of gene expression, chromatin remodeling, and cell cycle (Wahl
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In this current study we not only demonstrated
2022-02-17
In this current study, we not only demonstrated the growth-inhibitory effects of the 2nd generation analog SL-1-39 on the HER2+ breast cancer cells, MDA-MB-453 and SKBR3 (Table 1), but we also demonstrated that the decrease in cell number was associated with an interruption of GSK2801 australia pro
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br Hydroxamic acids br Inhibitors with reporting modalities
2022-02-17
Hydroxamic acids Inhibitors with reporting modalities Dual or more HDAC inhibitors Conclusion Finally, non-human HDAC such as Schistosoma mansoni HDAC8 are targeted for parasitic diseases and recent work highlight the interest of HDACs in viral infections. Despite their discovery in the
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In an effort to further
2022-02-17
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl group
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br Acknowledgements This work was financially
2022-02-17
Acknowledgements This work was financially supported by the National Natural Science Foundation of China (Grant No. 81803033) and the “Double First-Class” University project (CPU2018GF02). Introduction Atrial fibrillation (AF) is the most common progressive cardiac rhythm disorder. Studies ha
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br Significant efforts are currently focused on non dopamine
2022-02-17
Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) AMI-1 hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-containing synapses,
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lb100 Uracil DNA glycosylase UDG is a highly conserved damag
2022-02-17
Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA lb100 excision repair (BER) pathway which keeps the maintenance of genomic integrity and stability [[21], [22], [23]]. Howe
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br Excitatory amino acid transporter mediated glutamate tran
2022-02-17
Excitatory amino wdr5 transporter-mediated glutamate transport Early studies detailing the presence of uptake systems capable of transporting glutamate and aspartate into neurons and glia represented a critical step in the overall task of demonstrating that l-glutamate was indeed an endogenous e
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In fact changes in mitochondrial
2022-02-17
In fact, changes in mitochondrial dynamics directly affects many things including cellular metabolism [127], mitochondrial mass and turnover [128], mitochondrial transport, and calcium buffering [129]. Nigrostriatal DA neurons seem to have a preferential susceptibility to loss of Mfn2 when compared
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