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Studies have focused on a hydrophobic cage at the
2020-12-10
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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br Discussion Several DPP inhibitors are currently available
2020-12-10
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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To explore the mechanism behind differential
2020-12-10
To explore the mechanism behind differential activation kinetics, Marcott et al. (2018) manipulate local dopamine dynamics. They show that differences in dopamine concentrations are not responsible for different D2R activation kinetics, since D2-IPSCs reach similar amplitudes at different rates in N
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Although the formation and toxicity of DPC is theoretically
2020-12-10
Although the formation and toxicity of DPC is theoretically acceptable, it is difficult to evaluate the specific role of DPC and its repair enzyme MGMT in the cytotoxic and mutagenic effects because DPCs are estimated to constitute only 1%–3% of total DNA damage when EDTA synthesis are exposed to b
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G DH has gained interest because of its broad
2020-12-10
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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br Chagas disease and HAT drug R
2020-12-10
Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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TNF a major cytokine that is critical
2020-12-10
TNF-α, a major cytokine that is critical in acute and chronic inflammation, is responsible from chemotaxis, acute phase reactions and endothelial activation (Mahalingam and Karupiah, 1999). Our study showed that TNF-α is increased significantly in the pyelonephritic rats and montelukast displayed an
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Prostaglandins PGs are lipid mediators that exhibit
2020-12-10
Prostaglandins (PGs) are lipid mediators that exhibit a variety of physiological properties by interacting specific G protein-coupled receptors (GPCRs) [10]. PGD2 is synthesized from PGH2 through two distinct PGD synthases; lipocalin-type PGD synthase (L-PGDS) and hematopoietic PGD synthase (H-PGDS)
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Previously published data showed an interaction of
2020-12-09
Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino Dexmedetomidine HCl sequence
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It remains unclear how LINE RNA
2020-12-09
It remains unclear how LINE1 RNA-Nucleolin-Kap1 are targeted to the Dux cluster. LINE1-Nucleolin-Kap1 may have other interacting partners with DNA binding specificity. For example, YY1 has been implicated in targeting a repressive complex containing Nucleolin to the human DUX4 cluster (Gabellini et
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EphB and ephrinB mRNA levels were determined
2020-12-09
EphB4 and ephrinB2 mRNA levels were determined from three parts taken from each tumor, and each sample was analyzed in triplicate. The differences in the histoscores and mRNA levels of EphB4 and ephrinB2 were analyzed by Student's t test. The correlation coefficients were evaluated both by linear re
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Here we report for the
2020-12-09
Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a
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An Ubl modification requires several steps that
2020-12-09
An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo
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br Substrate characterization of candidate peptide reporters
2020-12-09
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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First of all it should be emphasized that although
2020-12-09
First of all, it should be emphasized that, although cPLA2α manifests a marked selectivity for phospholipids that contain AA at the sn-2 position, this does not mean in any way that, in cells, the enzyme cannot hydrolyze other fatty acyl residues to a significant extent even if this occurs at a lowe
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