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For further understanding of the interaction between these i
2021-11-15
For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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In an attempt to further optimize interactions in the
2021-11-15
In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou
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br Discussion Using HBV transgenic mice Kim et
2021-11-15
Discussion Using HBV transgenic mice, Kim, et al. first reported that the HBx gene caused HCC [34]. Since then, transgenic mice have become a useful experimental model for defining the molecular events of HBV hepatitis, and HBV-related hepatocarcinogenesis. In the present study, we first confirme
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br Materials and methods br Results br Discussion Directly m
2021-11-15
Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic Thalidomide is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate cancer. Howev
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Recently it was found that hypoxia results in the
2021-11-15
Recently, it was found that hypoxia results in the phosphorylation of β-catenin at Y654 in a Src-dependent manner (Xi et al., 2013). All β-catenin phosphorylated at this residue was found complexed with Hif1α and it was demonstrated that this β-catenin phosphorylation was required for Src to promote
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br Acknowledgements This work was supported
2021-11-12
Acknowledgements This work was supported by the Science and Technology Department of Hubei Province (No.2016CFB368) and the National Natural Science Foundation of China (No. 81201053). Introduction L-Glutamate (glutamate) is the most important excitatory neurotransmitter of the central nervou
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Many studies support that Gli
2021-11-12
Many studies support that Gli transcription factors are not solely regulated by Hh/smo signaling but are also influenced by crosstalk with other pathways, such as RAS, PI3K/AKT, transforming growth factor-b/SMAD, PKC, or extracellular signal-regulated kinase pathways which are downstream and indepen
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The finding that a peptide consisting
2021-11-12
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino ApexPrep DNA Plasmid Miniprep Kit ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective i
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Acknowledgments The authors thank Partners Healthcare for fi
2021-11-12
Acknowledgments The authors thank Partners Healthcare for financial support. This work was also supported in part by NIH Grant R01CA122608 to J.M.G.H. Introduction The phosphorylation of histone H3 is recognized as a hallmark of mitosis. Histone H3 phosphorylation at Thr3 (H3T3ph) acts as a mit
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The relaxant response to carperitide was
2021-11-12
The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is e
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Initially the synthesized compounds from
2021-11-11
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic Benidipine HCl synthesis havi
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In the present study we observed a decrease in
2021-11-11
In the present study, we observed a decrease in body weight gain in Tg rats. It is uncertain whether this effect is due to Denr, Gpr81, or Gpr109a. In this regard, Gpr81 mice have been reported to have reduced body weight gain [28]. Moreover, a small clinical study has reported that obese patients t
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The unique ability of R PabI to specifically
2021-11-11
The unique ability of R.PabI to specifically excise DNQX disodium salt from a palindromic sequence is based on a novel structural architecture that is distinct not only from other DNA glycosylases but also from other proteins [88]. In the absence of DNA, R.PabI forms a dimer with a central, highly
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br Glycoprotein Production br Strategies to Obtain Glycoprot
2021-11-11
Glycoprotein Production Strategies to Obtain Glycoprotein Compositional Homogeneity Glycoproteins are modified by glycosyltransferases and glycosylhydrolases in the ER and Golgi; however, the degree of remodeling for each glycan on each protein is not explicitly defined by a template (Moremen
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Tetrazole is one of the most
2021-11-11
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a
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