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br Materials and Methods br Acknowledgements br Introduction
2020-06-09
Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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br Conclusions br Introduction The terms
2020-06-09
Conclusions Introduction The terms endocrine active and endocrine disruptive have been used to describe an ever-expanding list of naturally-occurring and synthetic compounds that interact with mammalian hormonal systems, and in particular, the reproductive system. These compounds have been ass
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PRIMA-1MET br Materials and methods br Results br Discussion
2020-06-09
Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th
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In recent years there has been much interest within
2020-06-09
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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br Clinical studies br Practical
2020-06-09
Clinical studies Practical implications for young women Conclusion Research on the oncogenic mechanism of hormones has advanced dramatically in the latter years. The finding that progestogens are more powerful determinants of risk than estrogens in breast cancer has been added to advances i
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TKI discontinuation studies demonstrate that
2020-06-09
TKI discontinuation studies demonstrate that a portion of TKI-treated CML patients remain in remission for up to 3 years, although long-term risk assessment is still necessary (Bansal and Radich, 2016). The majority of CML patients depend on lifetime TKI treatment, and substantial efforts have been
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Furthermore the determination of downstream target genes
2020-06-08
Furthermore, the determination of downstream target genes induced by CdCl2 is noteworthy and can help to define its underlying carcinogenesis mechanism. Therefore, we evaluated c-fos and c-jun expression which are stimulated by estrogen through ERK/MAPK pathway. These are not only proto-oncogenes wh
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N Cyclopentylmethyl analog exhibited fold
2020-06-08
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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A number of chemical strategies have been developed to desig
2020-06-08
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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Metal ions are known not
2020-06-08
Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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Increased levels of PCNA monoubiquitination by UbL P express
2020-06-08
Increased levels of PCNA monoubiquitination by UbL73P expression in a damage-independent manner mimics the phenotype observed for USP1 knockdown (Huang et al., 2006, Jones et al., 2012). USP1 is the only DUB to date shown to remove ubiquitin from PCNA in vivo. This finding reveals the highly dynamic
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Experiments on the rat model of
2020-06-08
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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YM178 mg Drug drug interactions are frequently attributed to
2020-06-08
Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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We have previously disclosed the discovery
2020-06-08
We have previously disclosed the discovery of a 7-azaindole-3-acetic Autophagy Compound Library receptor CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to
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br Materials and methods br Results br
2020-06-08
Materials and methods Results Discussion This study is the first to our knowledge that describes upstream cis-elements and transcription factors that are important for Crm1 expression and that drive its high expression in cancer and transformed cells. Using deletion and mutation analysis we
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