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Covalent inhibitors are well suited for targeting the
2020-10-13
Covalent inhibitors are well suited for targeting the E1 salidroside receptor of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stab
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Enolase is an example of a moonlighting protein
2020-10-13
Enolase is an example of a moonlighting protein that displays multiple biological actions, including plasminogen, laminin, fibronectin, mucin and cytokeratin binding properties. It has also been described as a complement-evasion protein and as a protein capable of inducing neutrophil trap formation.
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br Materials and methods br Results
2020-10-13
Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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Prote MTX and MTXPGs block the activity of
2020-10-13
MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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The results described in the present study confirm key
2020-10-13
The results described in the present study confirm key restrictions on reaction conditions which must considered to maximize reactor productivity. Increased viscosity should be avoided for the amination of ketones by L-AmDH, as a 4-fold increase in viscosity can lower the reaction rate by as much as
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Temsirolimus br Results br Discussion Prostate cancer
2020-10-13
Results Discussion Prostate cancer dissemination and skeletal metastases represent major therapeutic challenges. Once the skeletal metastasis occurs, the incurable patient could just be symptomatically treated to alleviate the pain. Therefore it is of great necessity to disclose the molecular
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PMX 205 br DDR in atherosclerosis and vascular disease The C
2020-10-13
DDR1 in atherosclerosis and vascular disease The Canadian group of Bendeck, explored the role of DDR1 in repair following arterial injury in rats [30]. DDR1 protein levels, assessed via Western blots prepared from arterial extracts taken at various times after injury, showed DDR1 protein dramatic
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Cystatins are potent inhibitors of cysteine
2020-10-13
Cystatins are potent inhibitors of cysteine proteases from the C1A family. These inhibitors primarily reduce the activities of cathepsin L-like proteases, although high concentration of barley cystatin hampers the degradation of storage proteins caused by cathepsin F-like protein (HvPap-1) (Cambra e
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Previously to detect CDKL activity we used a radioactive
2020-10-13
Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti
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Cardiogenesis is enhanced with timely applicati http www ape
2020-10-12
Cardiogenesis is enhanced with timely application of Wnt pathway activators and inhibitors. A combination of Wnt/β-catenin signaling pathway activators such as CHIR99021 and inhibitors such as IWP-2 and IWR-1 have been found to be highly efficient cardiomyocyte differentiation protocols [27], [28].
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A more refined picture of cholinesterase activity patterns
2020-10-12
A more refined picture of cholinesterase activity patterns may be obtained by measuring ChE activity of the same sample before and after addition of certain cholinesterase inhibitors, with differential specificity for different components of total ChE activity, such as BW284c51 (BW1,5-bis-(4-allyldi
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Since the aggregation of neurotoxic forms of A
2020-10-12
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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In human neuroblastoma SH SY Y cells and in
2020-10-12
In human neuroblastoma SH-SY5Y ha tag and in lymphoma Jurkat cells, Yamanaka et al. [56] showed that exogenously added 24(S)-hydroxycholesterol could be efficiently esterified by ACAT1. These results suggest that both ACAT1 and ACAT2 can control the oxysterol levels by directly esterifying them, in
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On the other hand the
2020-10-12
On the other hand, the interaction of the Kaempferia parviflora extract with CYP3A was uncompetitive with a low Vmax value. In the in vivo study, the Kaempferia parviflora extract did not interfere with CYP3A activity throughout the entire duration of treatment. This is fortunate as CYP3A isoforms a
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br Asb Proteins and Mitochondrial Function Mitochondria are
2020-10-11
Asb Proteins and Mitochondrial Function Mitochondria are intracellular organelles in eukaryotic Mouse HGF / Hepatocyte Growth Factor Protein (His Tag) and are the main sites of oxidative phosphorylation and ATP production. In addition, mitochondria serve as signal transduction docking stations i
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