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In contrast to DDR the
2021-01-20

In Ro 48-8071 to DDR1, the role of oligomerization and/or clustering of DDR2 in mediating its interactions with collagen is less understood. Current data show that in DDR2, like in DDR1, (i) dimerization [7] and higher-order oligomerization of its ECD [11], [22] enhance its binding to collagen, and
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Our structures also provide new
2021-01-20

Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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Mass spectrometry has previously been used to examine
2021-01-20

Mass spectrometry has previously been used to examine the presence of Hyp in recombinant collagen, using hydrolysates to identify the individual imino acid, equivalent to an amino p2y receptor analysis [33], and also by analysis of mass changes to tryptic peptides [34]. The present study, however,
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br Results and discussion br Conclusion In
2021-01-20

Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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Iris domestica L Goldblatt Mabb
2021-01-20

Iris domestica (L.) Goldblatt & Mabb. (syn. Belamcanda chinensis L.) DC. (Iridaceae) occurs naturally in South and East Asia. Despite the fact that former monotypic genus Belamcanda has been included in the extended genus Iris, this classification has been questioned (Wilson, 2011; Mavrodiev et al.,
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Another potential source of variable affinities is inherent
2021-01-20

Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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Co operation or synergy between PKA and Epac has
2021-01-20

Co-operation or synergy between PKA and Epac has been recently reported in PCCL3 thyroid cell line in which cAMP is pro-mitogenic, in azd4547 to VSMC [19]. Our study demonstrates for the first time that PKA and Epac also synergise to inhibit cell proliferation in a cell type where cAMP in anti-mito
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br Materials and methods br Results br
2021-01-20

Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor 1478 recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell proliferation in bronchial carcinoids cells. The diverge
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br Results and discussion br
2021-01-20

Results and discussion Conclusions In this work, we have conjugated two thermophilic enzymes (i.e., AMY and LASPO) to iron oxide NPs through different conjugation strategies obtaining efficient biocatalysts. We have demonstrated that these NP-enzyme systems can be successfully activated by an
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Main Text Post translational modifications by ubiquitin
2021-01-19

Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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Compounds that interact with MDR can do so by
2021-01-19

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 tosylate and there was no observed reduction
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br Acknowledgments br The design of polyaromatic molecules
2021-01-19

Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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The preferences for source of FAs for DGAT and
2021-01-19

The preferences for source of FAs for DGAT1 and DGAT2 are related to their membrane topologies, subcellular locations, interactions with other proteins or organelles (discussed in the former section), and their differential expression, substrate specificities, and enzyme kinetics. According to UniPr
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The discoidin domain receptors DDR and DDR are receptor
2021-01-19

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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We further evaluated the functional relation between promote
2021-01-19

We further evaluated the functional relation between promoter regulation of the tumor suppressor genes and in fresh frozen, microdissected tumor tissue from 55 patient with clear cell renal carcinoma. In addition, normal-appearing tissue from the same patient taken distal of the tumor and later hi
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