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The cysteinyl leukotrienes cysLTs LTC LTD and LTE
2019-11-15
The cysteinyl leukotrienes (cysLTs) LTC, LTD, and LTE are increased in the airways of asthmatic subjects, with the ability to induce bronchoconstriction, vascular permeability, and mucus secretion., , , , CysLTs are well established as mediators of allergic rhinitis and asthma on the basis of the e
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In order to validate the
2019-11-15
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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The structure of the HOIP RBR LDD module bound
2019-11-14
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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br A brief history of RBR E s RBR
2019-11-14
A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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In the context of E ligase drug discovery
2019-11-14
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 Ack
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br Materials and methods br
2019-11-14
Materials and methods Results Because of the specific binding of DGKε to an arachidonoyl group, there was a particular interest to evaluate the behavior of 2-AG with this isoform of DGK. The substrate specificity and kinetic constants for DGKε has been recently reported [13]. Using the preferr
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In the present study we
2019-11-14
In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis jasplakinolide mg and leaves, we demonstrate that this sub-class of plant proteases is activat
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After activation AKT phosphorylates target proteins involved
2019-11-14
After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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The reaction of chitosan with DVS should take
2019-11-14
The reaction of chitosan with DVS should take place primarily through a nucleophilic attack of the vinyl sulfone groups to the amino groups in chitosan [39,50], although its hydroxyl groups can also be involved, as it happens when using agarose [35]. These reactions create very stable secondary amin
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Introduction Enzymes have higher selectivity specificity and
2019-11-14
Introduction Enzymes have higher selectivity, specificity and efficiency than chemical catalysts. Due to their properties and their green chemistry, biocatalysts are widely used in food, textile and pharmaceutical industry [1], [2]. A high efficient biocatalyst for industrial applications must be s
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In human neuroblastoma SH SY Y cells
2019-11-14
In human neuroblastoma SH-SY5Y Auranofin mg and in lymphoma Jurkat cells, Yamanaka et al. [56] showed that exogenously added 24(S)-hydroxycholesterol could be efficiently esterified by ACAT1. These results suggest that both ACAT1 and ACAT2 can control the oxysterol levels by directly esterifying the
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EBI and its ligand s EBI was found in a
2019-11-14
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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Previous in vitro studies have demonstrated
2019-11-14
Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM PD153035 hydrochloride
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Our ex vivo analysis demonstrates that
2019-11-14
Our ex vivo analysis demonstrates that IL-15 promotes CD122 expression in DGKζ-deficient CD8+ T cells. CD122, which forms a dimer with CD132 in response to IL-2 or IL-15, activates the JAK/STAT and PI3K/mTOR pathways. Whereas antigen-stimulated Disuflo Cy3 azide promote IL-2 sensitivity through up-r
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The crystal structure of full length CHK is still unsolved
2019-11-13
The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence al
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