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CaneCPI showed strong inhibitory activity against recombinan
2019-09-16
CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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Several main strategies for targeting E s described
2019-09-12
Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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Introduction Amphetamine AMPH methamphetamine MA and ethylen
2019-09-12
Introduction Amphetamine (AMPH), methamphetamine (MA), and 3,4-ethylenedioxymethamphetamine (MDMA) are widely abused psychoactive substances, with the basic chemical structure of phenylethylamine [1]. The abuse of these drugs is associated with psychostimulant, anorectic and hallucinogenic properti
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For the SAR optimization of the right hand
2019-09-12
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic Kinase Inhibitor Library mass moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was int
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Collectively the results presented here provide
2019-09-12
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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Distribution of DGTS in basidiomycete fungi has been demonst
2019-09-12
Distribution of DGTS in basidiomycete fungi has been demonstrated to be heterogeneous. In certain fungal taxons, such as Agaricales, Polyporales and Russulales, there are species that synthesize and species that do not synthesize DGTS that belong to the same order or even family (Dembitsky, 1996, Va
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Kumar et al studied Umbelliferone D galactopyranoside UFG be
2019-09-12
Kumar et al. studied Umbelliferone β-D-galactopyranoside (UFG) (benzopyrone), found in many plants exhibiting numerous pharmacological actions. The results of the study showed that UFG in a dose of 10, 20 or 40mgkg-1 per day, helps to prevent paw edema and arthritic score development for arthritis i
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In this study CK C prepared from BL
2019-09-12
In this study, CK1δ(ΔC) prepared from BL21(DE3)pλPP had the highest kinase activity among the three isoforms tested when using casein as a substrate. Therefore, CK1δ(ΔC) from BL21(DE3)pλPP has the potential to be a “phosphorylating reagent” that may be widely used in experiments of phosphorylation
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To better understand the mechanism
2019-09-12
To better understand the mechanism of splicing in CLCN1, we began by constructing a minigene spanning exons 5–7 of CLCN1, resulting in the synthetic CLCN1 (5–7) minigene. We also established a new assay using real-time reverse transcription (RT)-PCR, which can distinguish between splicing variants b
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br Results br Discussion The
2019-09-12
Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into Estradiol by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by their inhibi
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Many filarial species harbor an
2019-09-12
Many filarial species harbor an endosymbiotic bacterium of the genus Wolbachia. A recent investigation of Wolbachia distribution in 35 filarial species including 28 species and 7 genera and/or subgenera have shown that 37% of them harbor Wolbachia (Ferri et al., 2011). In filarial nematodes, Wolbach
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br Materials and methods br Results br
2019-09-12
Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated Viroptic guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and LTD4[9
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ID-8 br Roles of ERR in Physiology and Disease br
2019-09-11
Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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However with regard to the involvement of PEP
2019-09-11
However, with regard to the involvement of PEP in neoplastic processes, few studies and restricted to a very limited number of different tumors have been carried out [4], [18], [19]. Therefore, in order to ascertain the possible role of this enzyme in pathological proliferative tissues, in the prese
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In this study we have explored a functional role of
2019-09-11
In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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