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These data indicate that in the context of the
2020-10-30
These data indicate that, in the context of the N-terminal 42 amino acids of p53, threonine 18 is a substrate for phosphorylation by CK1 as mediated by prior phosphorylation of serine 15. To determine whether this is a property of full length p53, GST-p53 fusion proteins comprising the full length p
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br Acknowledgements This research was supported by
2020-10-30
Acknowledgements This research was supported by Slovenian Research Agency (ARRS). We thank prof. R. Marinšek Logar for helpful advice, Dr. T. Kranjc for help with data management, N. Vrhovnik and G. Lavrič for technical help with preliminary growth experiments and dr. J. Burkeljca for help with g
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Three kinase inhibitors dasatinib type I imatinib type II
2020-10-29
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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The acid base properties of the IL are important issues
2020-10-29
3. The acid-base properties of the IL are important issues to consider because protonation changes caused by Brønsted-acidic or basic ions may result in enzyme deactivation [29]. Thereby, the acid-base properties of the newly designed IL need proper control for enzymes by selection of appropriate ca
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We propose the following model for how B cell guiding
2020-10-29
We propose the following model for how B cell-guiding EBI2 ligand gradients are established in lymphoid tissues. CH25H and CYP7B1 are needed in radiation-resistant stromal cells, are abundantly expressed and active in CXCL13+ and CCL21+ FRCs, but not lymphocytes, and are poorly expressed in the inne
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In addition to cleaving ubiquitins
2020-10-29
In addition to cleaving ubiquitins off modified proteins, DUBs can also cleave between ubiquitin moieties within a polyubiquitin chain to edit the ubiquitin signal. DUBs employ different strategies to recognize polyubiquitin (Figure 1). DUBs that rely only on interactions on the S1 site tend to be c
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Compounds that interact with MDR can do so by
2020-10-29
Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant TMN 355 synthesis and there was no observed
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Proteases as multifunctional enzymes play key roles in contr
2020-10-29
Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on.
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br Materials and methods br Results br Discussion We initial
2020-10-29
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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br Acknowledgments br Introduction Inflammation is the prote
2020-10-29
Acknowledgments Introduction Inflammation is the protective reaction of the body to infection, injury, or irritation with the aim to remove harmful stimuli such as pathogens, damaged cells, or allergic irritants and to initiate the healing process. Inflammatory abnormalities play a crucial rol
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IT-901 While a number of studies have helped
2020-10-29
While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub IT-901 specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing substrate
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Several eukaryotic E enzymes including BRE RNF and
2020-10-29
Several eukaryotic E3 enzymes, including BRE1 [49], RNF8 [50], and RAD18 [24], [51], have been reported to partner with UBE2B in the ubiquitination of various targets. We examined the expression levels of these E3 enzymes in HONE1 and TW01 cells; RAD18 was highly expressed in these beta amyloid (da
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In a study carried out by Aunis et al
2020-10-29
In a study carried out by Aunis et al. the properties of soluble DBH and membrane bound were examined [23]. The membrane bound enzyme was shown in SU 9516 to the soluble form to have thermal denaturation at higher temperatures of 43.5–44°C. Similar discontinuities in the Arrhenius plots were obtain
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SP600125 ASC was reported as a potent antiviral and antifung
2020-10-29
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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Several highly potent CysLT receptor antagonists with large
2020-10-28
Several highly potent CysLT1 receptor antagonists with large structural Antagonist G have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazo
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