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Several CHK inhibitors have been
2020-08-31

Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indazo
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Ligand independent activation of neuronal nuclear
2020-08-31

Ligand-independent activation of neuronal nuclear estrogen receptors may also continue to occur in absence of ovarian estrogens. AF-1 requires intracellular kinase cascade-dependent phosphorylation of specific residues in the A/B domain of nuclear estrogen receptors (Le Goff et al., 1994; Kato et al
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Synthesis of and is described in Scheme Compounds and were
2020-08-31

Synthesis of 5–7, 12–14, and 18 is described in Scheme 3. Compounds 5–7 and 18 were prepared as outlined in Scheme 3a. Reaction of 4-bromomethylbenzoic ID-8 (36) with thionyl chloride yielded the corresponding acid chloride, which was converted to the corresponding amide 40a by the usual ammonolysi
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br Conclusions br Acknowledgements This work was supported b
2020-08-31

Conclusions Acknowledgements This work was supported by the Science and Technology Planning Projects of Guangdong Province (2014A020210027); the Major Scientific Research Projects of Universities in Guangdong Province (2016KZDXM042); the Natural Science Foundation of Guangdong Province (2015A0
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Although our knowledge of the biochemical and biological
2020-08-31

Although our knowledge of the biochemical and biological functions of E3 ubiquitin ligases has increased in B-cell malignancies, a deeper characterization of cell-context dependent substrate regulation and biological relevance is needed. The recent approval of a general proteasome inhibitor, VELCADE
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Consistent with a clear separation
2020-08-31

Consistent with a clear separation of biological function between ARISC and BRISC in cells, mutations in BRCC36 and Abraxas are prevalent in cancer genomes whereas mutations in KIAA0157 are rare. A survey of the Catalogue of Somatic Mutations in Cancer (COSMIC) consortium, revealed that to date, 37
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BMS-354825 Direct coupling between DNA methyltransferase
2020-08-31

Direct coupling between DNA methyltransferase enzymes and posttranslational modifications on histone proteins has been observed in mammals. For example, DNMT3A recognizes unmodified H3 through an ATRX-DNMT3-DNMT3L (ADD) domain, and its activity is inhibited by methylation of H3 at K4 (Li et al., 201
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NMR was employed for the determination of un ligated domain
2020-08-31

NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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In conclusion we propose that UBE T FANCT
2020-08-31

In conclusion, we propose that UBE2T (FANCT) mutations define a FA subtype. This is also a rare example of a mutated E2 enzyme causing an inherited human disorder, like UBE2A. The p.Gln2Glu substitution is probably hypomorphic, as indicated by the fact that a siUBE2T knockdown made AP65P-hTERT Cy7.5
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There have been reports regarding
2020-08-31

There have been reports regarding the use of enolases as novel vaccine candidates for A. suum, S. suis, T. pisiformis and T. multiceps on account of this enzyme class\'s critical role in plasminogen activation and migration across tissue barriers (Chen et al., 2012; Zhang et al., 2009; Zhang et al.,
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T cell infiltration is an important predictive
2020-08-28

T cell infiltration is an important predictive biomarker for the PD-1 blockade, and it is closely associated with a good prognosis. In our study, we found that T cells were low and exhausted within the tumor microenvironment and were distributed in the tumor margin. Anti-PD-1 treatment reduced PD-1
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Introduction Penetrator with Enhanced Lateral Effect
2020-08-28

Introduction Penetrator with Enhanced Lateral Effect (PELE) is a kind of ammunition which consists of a low-density material as the filling and a high-density material as the jacket [1,2]. When PELE impact target, the jacket is radially accelerated, expanded and fractured because of distinctive lat
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br Acknowledgments br Significance The mechanisms underlying
2020-08-28

Acknowledgments Significance The mechanisms underlying the adverse effects of Epo-stimulating agents on the reduced survival of cancer patients are not well understood. Here, we identified EphB4 as an alternative Epo receptor, which triggers Src/Stat3 signaling via EphB4. We also showed that r
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In this study we investigated whether the Ednra
2020-08-28

In this study, we investigated whether the Ednra signaling is involved in Hoxa9/Meis1-mediated leukemogenesis. We found an upregulation of Ednra in leukemic murine bone marrow (BM) 78416 overexpressing Hoxa9 and Meis1 compared to cells overexpressing Hoxa9 alone. We showed that overexpression of Edn
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br Results and Discussion br Conclusions Understanding the c
2020-08-28

Results and Discussion Conclusions Understanding the connections between function and fitness is a primary goal of many biological disciplines including systems biology and molecular evolution. While sound approaches have been developed to understand the connections between function and fitnes
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