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Here we found that these leukotriene antagonists also inhibi
2019-09-30
Here we found that these leukotriene antagonists also inhibit the effects of nucleotides acting at P2Y receptors in dU937 cells, which are known to express a number of nucleotide receptors, such as P2Y2 or P2Y4[30]. In an effort to characterize the P2 receptor subtypes subject to negative modulation
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br Materials and methods br Results and
2019-09-30
Materials and methods Results and discussion Acknowledgements This study was supported by the Open Project Program of the Key Laboratory of Mariculture & Enhancement of Zhejiang Province (No. 2016KF003), the Key Project of Zhejiang Province (No. 2016C02055-7), and the International Science
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br Prostaglandin D PGD is
2019-09-30
Prostaglandin D (PGD) is derived from the metabolism of arachidonic BW 723C86 hydrochloride mass by cyclooxygenases and downstream PGD synthases. In the immune system, PGD is mainly produced by mast cells but also although at lower levels, by macrophages and Th2 lymphocytes. PGD binds to three di
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Given its high frequency it
2019-09-29
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant RPC1063 mass to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been pro
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In this study we generated mice in
2019-09-29
In this study we generated mice in which the native Bcl6 locus was engineered to produce a form of Bcl6 containing a mutant RD2 domain that disrupts its repressor function. We found that RD2 domain is essential for pre-GC B cell differentiation and clustering into nascent GC within follicles, in par
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Modulating protein stability specifically inhibiting ubiquit
2019-09-29
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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The structure of the HOIP RBR LDD
2019-09-29
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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Most of the amino acid residues contacting the substrate
2019-09-29
Most of the amino phospholipase a2 inhibitor residues contacting the substrate are within the nucleotide-recognition lid (mauve or magenta in Fig. 4A). Two particularly important residues, W69 and Y76, are conserved in eubacteria and in some but not all of eight human AlkB homologs [52], [76] (Fig.
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Acknowledgments We are grateful to Dr Jean Marie Bernassau
2019-09-29
Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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The recombinant Scl collagen system has shown capability as
2019-09-29
The recombinant Scl2 collagen system has shown capability as a biomaterial as well because of its adaptability and scalability. Scl2 was functionalized to crosslink into a hydrogel without disrupting its triple helix [130]. The Scl2–hydrogel crosslinking also did not disrupt cell adhesion and integr
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Addition of deoxyuridine to CY cultures led to a significant
2019-09-29
Addition of deoxyuridine to CY11 cultures led to a significant decline in the amount of uracil-DNA (Fig. 5). Deoxyuridine effectively induces the deo operon and is efficiently degraded to uracil and deoxyribose 1-phosphate by the deoA gene product, thymidine phosphorylase; a minor percentage of deox
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br Rationale Recently we have shown that the nasal CysLT
2019-09-29
Rationale Recently we have shown that the nasal CysLT2 receptor localized exclusively in blood vessels and the expression level of the CysLT2 receptor in patients with nasal allergy was higher than that in patients with non-allergic rhinitis (Shirasaki et al. Allergol Int 2013). We hypothesized t
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br Introduction Benzanthrone BNZ is a dye
2019-09-29
Introduction Benzanthrone (BNZ) is a dye intermediate used in the synthesis of number of polycyclic vat and disperse dyes. It has been detected as an environmental pollutant in urban ambient air particulates, originating from furnace effluents, municipal refuge, wood and coal combustion and autom
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br Use of CDK inhibitors in CLL today There
2019-09-29
Use of CDK inhibitors in CLL today There has been explosive development of novel therapeutics for CLL in the last decade and a massive transformation of practice is underway [75]. Most of this development and excitement revolves around B-cell receptor (BCR) signaling inhibitors: the Bruton tyrosi
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Acidic substituents showed moderate biochemical activity but
2019-09-29
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic Koumine mass were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemica
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