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As compared with the broad spectrum of chemicals
2019-09-19
As compared with the broad spectrum of chemicals known to serve as the ligands for PXR and CAR, the ligands of VDR are previously restricted to VD3 as well as its hydroxylated metabolites and the secondary bile Obeticholic Acid LCA. Recently, the VDR-binding capacities of more compounds have been d
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In the course of our program
2019-09-19
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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br Signaling of DDR receptor and
2019-09-18
Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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br Chagas disease and HAT
2019-09-18
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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br Materials and methods br Results and
2019-09-18
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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Introduction The first reference to a
2019-09-18
Introduction The first reference to a possible involvement of orexins in the effects of drugs of abuse appeared in 2003 and showed that orexigenic peptide neurons respond to the chronic administration of morphine followed by abrupt withdrawal symptoms caused by opioid receptor antagonists (Georgesc
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Interestingly from our consensus SBVC protocol only few comp
2019-09-18
Interestingly, from our consensus SBVC protocol only few compounds (less than 150) have been scored with a full ‘ consensus’. That means that these compounds appear in the top 5% of the database when ranked by every scoring function independently. After visual inspection, we have realized that two a
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br Substrate characterization of candidate peptide reporters
2019-09-18
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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To our knowledge immunohistochemical analysis for proGRP was
2019-09-18
To our knowledge, immunohistochemical analysis for proGRP was done in 5 cases [9], [10], [17], [18]. Takagi-Takahashi et al. reported that the tumor Cucurbitacin I mass were positive for proGRP in one case [9]. Yamaguchi et al. also showed that tumor cells in two patients of ES/PNET with elevated se
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The modification of proteins with the small amino acid
2019-09-17
The modification of proteins with the small 76-amino AG-490 protein ubiquitin (Ub) plays a central role in many key cellular processes. Ubiquitylation of a target protein requires the concerted action of a cascade of three enzymes (Figure 1). The ubiquitin-activating enzyme (E1) catalyzes the forma
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Mother rats acutely treated with
2019-09-17
Mother rats acutely treated with quinpirole (0.5 and 1.0 mg/kg) decreased the pup exploration time but increased the object exploration, so they showed a significantly lower pup preference ratio. They also showed impaired maternal performance in the home cage, consistent with our previous study (Zha
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CYP A is involved in the metabolism of
2019-09-17
CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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As the principal receptors for regulating
2019-09-17
As the principal receptors for regulating the inflammatory process in mammals, CXCR1 and CXCR2 have an important role in regulating the trafficking of phagocytes such as neutrophils, monocytes and macrophages (Viola and Luster, 2008). The evidence gathered to date from fish studies are in agreement
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T cell infiltration is an important
2019-09-17
T cell infiltration is an important predictive biomarker for the PD-1 blockade, and it is closely associated with a good prognosis. In our study, we found that T cells were low and exhausted within the tumor microenvironment and were distributed in the tumor margin. Anti-PD-1 treatment reduced PD-1
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In the particular case of
2019-09-17
In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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