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Classical DHFR inhibitors such as methotrexate MTX bind
2020-09-29
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Vitamin B12 residues as well as hydrophobi
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The binding of collagen X
2020-09-29
The binding of collagen X to DDR2 differs from the binding of collagen X to α2β1 integrin in that the triple helical conformation is essential for DDR2 binding. We previously reported that heat denatured pepsinised collagen X supported cell adhesion via α2β1, indicating that the triple-helical confo
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The second DDR binding partner identified
2020-09-29
The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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Second when considering the Poisson point process the high
2020-09-29
Second, when considering the Poisson point process, the high-density or large-radius limit of the percolation probability tends to 1 exponentially fast and is governed by the isolation probability. In the random environment, the picture is more subtle since the regime of a large radius is no longer
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From materials science it is known that the differences
2020-09-29
From materials science, it is known that the differences in the annealing temperature is the main factor that mostly influences La (Takai et al., 2003, Cançado et al., 2006). In analogy, controlling the pyrolysis temperature and SANT-1 during residues burning might be a key aspect to reproduce the
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Protein kinase casein kinase CK comprises
2020-09-28
Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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br Conflicts of interest br Acknowledgements This study was
2020-09-28
Conflicts of interest Acknowledgements This study was funded by Kuwait University Research Administration (Project MI03/10). Introduction Epidemiological, experimental and biologic plausibility support a cardioprotective effect of estrogens in women [1]. Indeed, women are protected until t
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her2 inhibitor SS is a high grade malignant soft tissue sarc
2020-09-28
SS is a high-grade malignant soft tissue sarcoma accounting for 5%–10% of soft tissue sarcomas. After RMS, SS is the most common sarcoma in children, adolescents and young adults [9]. SS originates primarily in the lower (62%) and upper (21%) extremities but may occur at any anatomic site [9], [10].
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In looking at exist http www apexbt
2020-09-28
In looking at existing FGE substrates from other organisms, there are no reported effects on conversion efficiency of the general XCXPXRX pattern with respect to placement within or at the N′ or C′ terminus of polypeptides, and it has been suggested that the aldehyde formation is independent of the
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Therefore HNE is an attractive
2020-09-28
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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br Perspective and conclusion Collagen Toolkits
2020-09-28
Perspective and conclusion Collagen Toolkits II and III have been used to determine the R406 free base synthesis for DDR1 and DDR2, and the main binding site is the GVM-GFO motif [103,108]. The co-crystal structure of the DS domain of human DDR2 bound to a synthetic collagen-like peptide contain
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The potential existence of ER stress was first examined in
2020-09-28
The potential existence of ER stress was first examined in EVTs in placental bed biopsy specimens obtained from pregnancies complicated by early-onset preeclampsia. It was then tested whether ER stress can modulate MMP-2 activity before elucidating the role of proinflammatory cytokines in the induct
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In contrast to SQLE HMGCR could be efficiently
2020-09-28
In contrast to SQLE, HMGCR could be efficiently degraded in VKGILS-NH2 lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our recently
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Among the Ub interactions observed in
2020-09-28
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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FOX proteins constitute a large class of transcription facto
2020-09-28
FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO
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