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Aspergillus nigerA niger is another filamentous fungus in wh
2019-12-16

Aspergillus nigerA. niger is another filamentous fungus, in which alternative dehydrogenases have been described. Filamentous fungi are a very important group of microorganisms that are used in industry (O’Donnell et al. 2011). Biotechnological production processes using these organisms are often hi
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br Materials and methods br Results br Discussion
2019-12-16

Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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SANT-1 br Results br Discussion The sequence
2019-12-16

Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into SANT-1 by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by their inhibition
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Nuclear export mediated by CRM is initiated by
2019-12-16

Nuclear export mediated by CRM1 is initiated by an interaction between RanGTP and the HEAT9 loop of CRM1, triggering a conformational change in the NES binding site that permits NES–cargo protein binding (Dong et al., 2009, Fung and Chook, 2014). Our docking simulation results predicted that DP2392-
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In the intestine absorbed cholesterol
2019-12-16

In the intestine, absorbed cholesterol can either be esterified by ACAT2 (Soat2) and packed into chylomicrons, transported back to the intestinal lumen by ABCG5/ABCG8, or it can be transported into HDL by ABCA1. ACAT2 is confined to enterocytes and hepatocytes and esterifies cholesterol for intracel
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br Conclusions br Acknowledgements br
2019-12-16

Conclusions Acknowledgements Protein tyrosine kinases (PTKs) of Src family are important components in cellular signal transduction pathways that couple diverse extracellular signals to appropriate cellular responses . Their activities are tightly regulated in the cells and aberrant activati
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ERR and ERR share high sequence homology
2019-12-14

ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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br Role of ERK signaling in preventive and therapeutic
2019-12-14

Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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The present study showed evidence that the AT and
2019-12-14

The present study showed evidence that the AT1 and the ETA receptors were not expressed near or on the plasma membrane as monomers, but also as possibly constitutive dimers and tetramers. For both receptors, the proportion of monomers, dimers and tetramers were unaffected by their respective agonist
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The strand domain swap in the UbV XR dimer appears
2019-12-14

The β strand domain swap in the UbV.XR dimer appears to be a unique arrangement for a Ub-based dimer. In solution, free Ub has a KD of ∼5 mM for the monomer-dimer equilibrium, and the two subunits in the dimer adopt a range of relative orientations involving residues from Ub’s β sheet (Liu et al., 2
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Predictions of enzyme topology for DGAT
2019-12-14

Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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BI-9564 mg br Results br Discussion The ubiquitin system
2019-12-13

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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Ponesimod australia br Materials and methods br Results br
2019-12-13

Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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Immune modulation by steroid hormones
2019-12-13

Immune modulation by steroid hormones is a rather new aspect of the research on endocrine interactions in lower vertebrates (Harris and Bird, 2000). In the classical view, steroids exert their effects by binding to specific intracellular receptors that function as ligand-activated transcriptional re
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All known vertebrate TRIMs are categorized
2019-12-13

All known vertebrate TRIMs are categorized in 11 distinct subclasses depending on the types of domains present at their carboxyl-terminals (Fig. 3) [29], [35]. Beyond conserved N-terminal domains, it is the C-terminal that provides specificity of interactions with other proteins. The subclass IV for
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