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When six chemical inhibitors were incubated with TRB or
2019-07-27
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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Several main strategies for targeting E s
2019-07-27
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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Despite the important agronomic traits regulated
2019-07-27
Despite the important agronomic traits regulated by SUMO, most research studies on SUMOylation have been mainly limited to model plants, such as Arabidopsis and rice (Wang et al., 2011), due to the lack of molecular tools specific to other economically relevant plants. On the other hand, plants harb
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br Experimental methods br Results
2019-07-27
Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.
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AMD is equally active against a broad
2019-07-27
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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Within the Class II receptors the Type I IFN
2019-07-27
Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem VU 591 hydrochloride of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely related,
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Collagen compaction and alignment are
2019-07-26
Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano
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Cell migration and invasion are central processes in the dev
2019-07-26
Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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Agglutinin like sequence ALS gene is
2019-07-26
Agglutinin-like sequence (ALS) gene is well-characterized gene family in candidiasis due to its importance in pathogenicity of C albicans. Previously, C. albicans ALS1 gene product was reported as cell surface protein that mediates adherence to endothelial and epithelial SBI-0206965 in vitro and du
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br Materials and methods br Results The monoclonal antibody
2019-07-26
Materials and methods Results The monoclonal antibody (mAb), 12G5, reacts specifically with the human fusin protein and recognizes the protein on many T-cell lines such as the SUP-T1 E-64-d (Endres et al., 1996). As shown in Fig. 1, AMD3100 at 25 μg/ml completely inhibited the binding of the
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The inhibition of FAS by C produces an accumulation of
2019-07-26
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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Previously we have shown that complexes of protein
2019-07-26
Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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br Conclusions In a former
2019-07-26
Conclusions In a former study we compared the modulating potential of halogenated 1H-benzimidazole derivatives towards CK2 catalytic subunits. Now we were interested if similar differences are also obtained using completely different substances. Some of these natural occurring compounds were alre
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Protein kinase casein kinase CK comprises
2019-07-26
Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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RCT pathway plays a critical role in the maintenance
2019-07-26
RCT pathway plays a critical role in the maintenance of cholesterol homeostasis by facilitating the cholesterol clearance and cholesterol efflux (Levinson & Wagner, 2015). In the process of RCT, ABCA1 and ABCG1 played as crucial regulators in cholesterol efflux (Yasuda et al., 2011). Compared with h
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