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Herein we explored by docking studies the effectiveness of r
2019-10-17
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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br Acknowledgements br This work was supported by
2019-10-17
Acknowledgements This work was supported by grants from the National Natural Science Foundation of China (Grant No.: 30260088) and the prophase research for National “973” Project of China (Grant No.: 2007CB116203). The DNA sequences of Hbvp1 and the Hbvp1 promoter were deposited in GenBank, an
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alkaline phosphatase inhibitor br CDK Inhibitors for the
2019-10-17
CDK Inhibitors for the Treatment of inflammatory Diseases Several CDKs have been implicated as regulators of inflammatory gene expression. It will thus be very important to determine the relative contributions of the various CDKs and their kinase function on a systematic basis. This work will be
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Findings from the present study indicate
2019-10-17
Findings from the present study indicate that CRF1 receptors are especially important in fear acquisition. CP154,526 given before acquisition training, at least partly, reinstated the fear-potentiated startle response and blocked the development of contextual conditioned fear in SERT−/− rats. CP154,
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Activating GSK signaling to inhibit PK signaling during isch
2019-10-17
Activating GSK3β signaling to inhibit PK signaling during ischemia/reperfusion (I/R) is protective of WM ischemic injury. Glycogen synthase kinase (GSK3), which was the first substrate identified for AKT [44], is inhibited by AKT phosphorylation at positions S9 and S21 [45]. When GSK3β is active, it
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An ideal CHK inhibitor would be
2019-10-17
An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th
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br Materials and methods br Results To investigate the
2019-10-17
Materials and methods Results To investigate the effect of 17βE on cell proliferation in the human renal tubular epithelia, BrdU uptake was measured in HRTEC primary and 3D-HRTEC cultures, allowing determination of the DNA replication rate. Representative microphotographs show BrdU uptake in H
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ERR and ERR share high sequence homology
2019-10-17
ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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The T cell receptor TCR pathway is associated with T
2019-10-17
The T cell receptor (TCR) pathway is associated with T cell activation and differentiation. When specific antigen peptides are recognized by the TCR, lymphocyte-specific protein tyrosine kinase (lck) phosphorylates the immune-receptor tyrosine-based activation motifs (ITAMs) of the TCR-CD3 complex a
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br Funding This work was supported
2019-10-17
Funding This work was supported by intramural funding of the Department of Internal Medicine I-Cardiology, University Hospital Aachen, RWTH Aachen. Acknowledgments Introduction Cyclic adenosine monophosphate (cAMP) is a central second messenger that controls a plethora of vital functions.
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In conclusion we designed novel E inhibitors
2019-10-17
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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Information on the mechanism by which parasite infections pr
2019-10-16
Information on the mechanism by which parasite infections promote ECM degradation is limited (McKerrow et al., 1983; Andrade, 1994; Lu and Lai, 2013; Thibeaux et al., 2014). The interaction of plasminogen-plasmin with proteins of microorganisms, including bacteria, has been suggested to play a key r
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serotonin receptor The current study demonstrates a link bet
2019-10-16
The current study demonstrates a link between heme metabolism and mitochondrial Co-I, which deficits instigate abnormalities in the metabolism of heme and its downstream targets both in-vitro in patients and healthy subjects derived LCLs and in-vivo in brains of SZ-rat model. A further study of the
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br RING dimerization RING type
2019-10-16
RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain LB-100 pathway (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC
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The occurrence of three Ag NORs
2019-10-16
The occurrence of three Ag-NORs per metaphase and/or a maximum of three nucleoli per nucleus in most of the varieties may be explained by chromosomal rearrangements or unequal crossing-over events that induce the deletion of the fourth active rDNA loci. Also, the chromosome pair that showed less int
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