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Currently much effort has been made to design
2020-04-06
Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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CFSs are recognized as a driver of
2020-04-06
CFSs are recognized as a driver of genome instability in human cells and are hotspots for deletions or translocations in cancers (Richards, 2001). The generally accepted model for their expression is that the CFS locus shows a delay in chromatin condensation in early mitosis caused by the persistenc
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Several models show the MAPK pathway involving p as the
2020-04-03
Several models show the MAPK pathway involving p38 as the Z-Ligustilide pathway in pro-inflammatory responses, with the ERK pathway involvement primarily devoted to cell growth and differentiation events (Lai et al., 2001, Widmann et al., 1999). The results of the current study would contradict thos
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p kip is a member
2020-04-03
p27kip1 is a member of the cyclin-dependent kinase (CDK) inhibitor family that acts as a potent tumor suppressor in a variety of human cancers and negatively regulates the transition of cells from the G1 to S phase of the cell cycle, protects against inflammatory injury and promotes epithelial diffe
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Park et al expanded their
2020-04-03
Park et al. [34] expanded their own model as hydrogen- bonding lattice fluid EOS (NLF-HB) [35] for calculating the activity coefficients of aqueous amino Pyronaridine Tetraphosphate solution. Further, Pazuki et al. [36] extended the perturbed hard chain theory which has been proposed by Beret and Pr
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Our previous studies have shown that in a preimplantation mo
2020-04-03
Our previous studies have shown that in a preimplantation mouse embryo the proportion of inner to outer cells (i.e. precursors of ICM and TE, respectively) is regulated by a different frequency of differentiative cell divisions at the 8- and 16-cell stages. Low number of inner blastomeres generated
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br Materials and Methods br Author Contributions
2020-04-03
Materials and Methods Author Contributions Conflicts of Interest Acknowledgments This work was sponsored by the National Natural Science Foundation of China (81802517), the Integrated Traditional Chinese and Western Medicine of Shanghai (ZHYY-ZXYJHZX-1-03), the Clinical Research Program
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Further modifications on the position of
2020-04-03
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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br Oxidoreductase like MEM for prodrug activation
2020-04-03
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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We have previously reported DAPK inhibitors discovered
2020-04-02
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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br Acknowledgments The authors thank Elisabete Lepera and
2020-04-02
Acknowledgments The authors thank Elisabete Lepera and Rosana Silva for technical support. The study was supported by FAPESP, CNPq and PADC/FCF-UNESP. T.T. Miguel was the recipient of a FAPESP (Proc. 05/05171-1) and R.L. Nunes-de-Souza of a CNPq (Proc. 303580/2009-7) fellowship. Introduction
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br Introduction The offspring of rodents emit
2020-04-02
Introduction The offspring of rodents emit vocalizations when isolated from their dam. The majority of vocalizations by rat pups are in the ultrasonic band frequency of 30–50 kHz (Insel et al., 1986). Maternal separation-induced ultrasonic vocalizations are believed to represent distress signals
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After the policy of the current British Commonwealth countri
2020-04-02
After 1915, the policy of the (current) British Commonwealth countries (including Britain, Canada, Australia, India, New Zealand and South Africa) regarding the dead, was to ensure that as far as possible, whether identified or not, all recovered bodies would be given individual graves, with standar
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Finally considering the encouraging inhibitory
2020-04-02
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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br Cholesterol handling in the arterial
2020-04-02
Cholesterol handling in the arterial wall cells Foam cell formation in the arterial intima is a major hallmark of early-stage atherosclerotic lesions, which is attributed to uncontrolled uptake of modified lipoproteins, excess cholesterol esterification and impaired cholesterol release [44]. As
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