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Resistance to SP is linked to
2020-07-21
Resistance to SP is linked to point mutations that accumulate at several sites in the dihydrofolate reductase (dhfr) and dihydropteroate synthase (dhps) CX4945 of P. falciparum (Roper et al., 2003). These mutations have been identified in codons 16, 51, 59, 108, and 164 in the dhfr gene and codons
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The potential off target activity of
2020-07-20
The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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br Structural and biochemical features of
2020-07-20
Structural and biochemical features of pol X family polymerases The X-family DNA polymerase (polX) is specialized in DNA repair. This family is composed of four different DNA polymerases: pol β, pol λ, pol μ and TdT. Only three members of the polX family possess an N-terminal BRCT (BRCA1 carboxy-
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It was demonstrated that the
2020-07-20
It was demonstrated that the addition of 10-fold excess of α-synuclein without modifications (with respect to the molar concentration of tetrameric GAPDH) leads to partial inactivation of GAPDH after 1-h incubation by 20% (Fig. 4, curve 2) in metabolic enzymes to insignificant decrease of the specif
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Considering the protumoral functions of TAMs new therapies a
2020-07-20
Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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Proteases as multifunctional enzymes play key roles
2020-07-17
Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on.
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Due to the results of
2020-07-17
Due to the results of the experiment we decided to deploy our cloud service infrastructure with two platform-independent servers instead of one or three. This decision was based on two factors: (a) the use of more than one server is useful to avoid a bottleneck in the system, and (b) using more than
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Our present results support a major role of EP
2020-07-17
Our present results support a major role of EP1 receptors in peripheral heat sensitization and a smaller contribution to central heat sensitization but no contribution to mechanical sensitization. While the contribution of peripheral EP1 receptors to heat hyperalgesia is in good agreement with the a
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The key difference between the membrane
2020-07-17
The key difference between the membrane zymography and classical measurements of enzyme activities in soil slurries is the enzyme-substrate accessibility. Classical enzyme assays maximize access of substrate to all potentially reactive enzyme sites by ensuring sample destruction and detachment follo
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Given its high frequency it is not
2020-07-17
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant INDY to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been proved effe
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In some pancreatic and non pancreatic tissues the
2020-07-16
In some pancreatic and non-pancreatic tissues, the chloride and calcium channels are heavily regulated by phosphorylation by protein kinases, such as PKC, cyclic AMP-dependent protein kinase (PKA), PKCaMKII, PI3K and protein tyrosine kinases [7,36,37]. Since the interaction of triterpenes with recep
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br Target enzyme attributes and substrate peptide selection
2020-07-16
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast m
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br Conclusion br Experimental NMR spectra
2020-07-16
Conclusion Experimental NMR spectra were recorded on a Jeol spectrometer at either 270 or 400 MHz for 1H spectra and either 68 or 100 MHz for 13C spectra. All chemical shifts are quoted in ppm relative to tetramethylsilane. In the assignment of signals the abbreviation DHN is used for 2,3-dihy
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The generation of ROS in addition to
2020-07-16
The generation of ROS, in addition to eliciting oxidative stress, is an important proapoptotic signal (Ott et al., 2007). Apoptosis is clearly associated with the production of ROS, since ROS generation occurs in the mitochondrial respiratory chain and disturbs mitochondrial homeostasis, which plays
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Elevated DPP activity has been strongly associated
2020-07-16
Elevated DPP-4 activity has been strongly associated with diabetes mellitus, IR (Röhrborn et al., 2015), metabolic syndrome (Lamers et al., 2011) and inflammation (Zhong et al., 2015). However, report has it that GC exposure increases DPP-4activity in thymocyte homogenates (Kraml et al., 2003) but t
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