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A structural explanation for how RBR RING
2020-06-10
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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The best characterized APC C
2020-06-10
The best-characterized APC/C substrates are recruited via various linear motifs (e.g., D boxes, KEN boxes, and ABBA motifs) that serve as degrons, binding to distinct regions of the β-propeller domain of a coactivator (Figure 1, Figure 3B) (reviewed in [44]). In addition, D boxes also simultaneously
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Poxviruses have double stranded DNA dsDNA genomes yet
2020-06-10
Poxviruses have double-stranded DNA (dsDNA) genomes, yet they replicate within the cytoplasm. Poxviruses that cause human disease include monkeypox virus (Reynolds et al., 2004), molluscum contagiosum virus (Hanson and Diven, 2003) and variola virus (VARV), the cause of smallpox, a disease eradicate
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br Introduction The discoidin domain receptors DDRs DDR and
2020-06-10
Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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The primary aim of this
2020-06-10
The primary aim of this study was to evaluate DAPK methylation as a tumor marker which is not only detected in the primary tumor but also in the serum of patients. We used matched pre-operative serum samples to determine the correlation of tumor and serum results. Despite an equal methylation freque
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A range of therapies exists for the treatment of inflammatio
2020-06-10
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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Moreover recent structural studies of
2020-06-10
Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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Several highly potent CysLT receptor antagonists with large
2020-06-10
Several highly potent CysLT1 receptor antagonists with large structural GPCR Compound Library have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, a
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2020-06-10
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase bms webpage receptor [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumou
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In solid tumors such as those in breast and pancreatic
2020-06-10
In solid tumors, such as those in breast and pancreatic cancer, infiltrating CD68+ or CD163+ tumor-associated macrophages (TAMs) correlate with poor outcome (DeNardo et al., 2011, Kurahara et al., 2011, Shabo et al., 2008). The tumor-promoting function of TAMs is based on their capacity to secrete p
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The radial distribution function is given by
2020-06-10
The radial distribution function, , is given by: For pure components and pseudo-components, the constants a and b are calculated as:whereand Tc, Pc and ω are the critical temperature, critical pressure and acentric factor, respectively. Parameters a and b for mixtures are calculated from those of
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Khan et al studied the effects of
2020-06-10
Khan et al. studied the effects of two structurally divergent coumarins viz calipteryxin 3 and (3′S,4′S)-3′,4′-disenecioyloxy-3′,4′-dihydroseselin 4 from Seseli recinosum, in lipopolysaccharide (LPS)-stimulated murine macrophages. The study revealed that calipteryxin and (3′S,4′S)-3′,4′-disenecioylo
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br Results and discussion br Conclusion
2020-06-09
Results and discussion Conclusion Analogues of 1,2,4-triazole and 1,3,4-oxadiazole have been designed, synthesized and characterized. To avoid late stage failure, it is important to study the preliminary pharmacokinetic parameters. The results of pharmacokinetic data suggested that, all molecu
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With regards to what might
2020-06-09
With regards to what might represent a typical “baseline” ChE (or AChE) activity in Saccostrea sp., it Angiotensin Fragment 1-7 acetate should be remembered that the observed enzyme responses were obtained in laboratory exposures, over a narrow experimental window (96h), with specimens collected ov
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Importantly we observed significantly the
2020-06-09
Importantly, we observed significantly the reduced myocardial infarct size, the improved left ventricular function and the inhibited fibrosis after I/R with oral GA-BH4 supplementation before ischemia (Fig. 1, Fig. 2, Fig. 3). Usually, there is a view that the antioxidation induced by reducing agent
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