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Nevertheless because of the preclinical work and the interfe
2021-05-06
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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ERR is expressed in several adult and embryonic tissues but
2021-05-06
ERRγ is expressed in several adult and embryonic tissues but its biological role is still largely unknown [21]. Overexpression of ERRγ in breast cancer correlates with a favorable outcome [22]. In addition, ERRγ has been reported to inhibit the growth of prostate tumor hif inhibitor [23]. In this s
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Our observation that nuclear but not cytoplasmic EP
2021-05-06
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant Deacetylase Inhibitor Cocktail synthesis whereas cytoplasmic EP4 was commonly observed [
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Next we compared the protease specificity of viruses
2021-05-06
Next, we compared the protease-specificity of viruses NS116-GFP/AE and NS116-GFP/AT for trypsin, neutrophilic elastase or supernatant of human neutrophils. For later purposes, we determined the viral yield in a co-cultivation system of infected Vero Berberine with human neutrophils. The NS116-GFP/e
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Three kinase inhibitors dasatinib type I imatinib type II an
2021-05-06
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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4E1RCat How does an increase in E affinity for
2021-05-06
How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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br Results br Discussion The ubiquitin system has in recent
2021-05-06
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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br Experimental Procedures br Author
2021-05-06
Experimental Procedures Author Contributions M.B., with input and help from T.T.H., conceived the project, designed and performed the experiments, analyzed the data, and wrote the manuscript. B.B.B. and F.D.M. synthesized the wild-type and (nonhydrolyzable, NH) Ub tetramers and contributed Fig
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In most cases patients will not present immediately
2021-05-06
In most cases, patients will not present immediately after SM exposure because SM-induced clinical symptoms typically occur after a latency period of several hours [8], [9], [10]. When they do present, the detection of free, unbound alkylating agent is highly unlikely. For this reason, available rap
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ASC was reported as a
2021-05-06
ASC was reported as a potent antiviral and antifungal agent, and its derivatives could modulate a variety of physiological activities, such as anti-tumor, anti-metastatic, and anti-diabetic activities in animals. Mie Tsuruga et al. found that 4-o-methylascochlorin had immunosuppressive activity, but
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br Results br Discussion The importance of mitochondria for
2021-05-06
Results Discussion The importance of mitochondria for the initiation and progression of tumorigenesis is now emerging. It is evident that, despite the well-known Warburg effect, tumors have active mitochondrial bioenergetic metabolism (Marin-Valencia et al., 2012, Hensley et al., 2016). Disrup
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br Conclusions This study showed that in
2021-05-05
Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC Losartan mg with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed at the promoter
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The mechanism by which OC
2021-05-05
The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b
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The ADME profile of AAT
2021-05-05
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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br Acknowledgment We thank Professor Yuh Chang
2021-05-05
Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, ach
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