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br Introduction Malaria remains a serious parasitic disease
2020-07-28
Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans
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br Biological evaluation br Molecular modelling studies
2020-07-28
Biological evaluation Molecular modelling studies Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were perfo
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atp 4 br Use of recombinant collagen to study DDR
2020-07-28
Use of recombinant collagen to study DDR–collagen interactions Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to
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To test our hypothesis that the relative stability of
2020-07-28
To test our Ryuvidine that the relative stability of the DFG-Asp-out conformation is related to promiscuity, we looked at data available in the PKIS2 set for a kinase that was tested in a state stabilized in DFG-Asp-in and the DFG-Asp-out conformation. We found data for activation loop phosphorylate
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amikacin sulfate We detected full length DDR in the
2020-07-28
We detected full-length DDR1 in the soma of only certain astrocytes and oligodendrocytes, indicating that this receptor may be expressed in these cells only under particular circumstances, i.e., after activation of the cells by exogenous molecules such as growth factors and cytokines (Matsuyama et a
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In order to further dissect the features underlying partner
2020-07-28
In order to further dissect the features underlying partner recognition by CaM, we undertook a quantitative study aimed at characterizing the complexes CaM–Can (n=0–4) involved in target interaction. Using fluorescence polarization, we analyzed the interaction between SynCaM, the product of the synt
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A cocktail approach can detect the activities of
2020-07-28
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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Regarding the involvement of CRF receptors located within th
2020-07-28
Regarding the involvement of CRF receptors located within the PAG on fear/anxiety-related responses, previous studies have shown that intra-dPAG infusion of h/rCRF (Martins et al., 2000) and ovine CRF (Borelli and Brandão, 2008) increase anxiety-like behaviors in rats exposed to the elevated plus ma
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What would be the possible off
2020-07-27
What would be the possible off-target effects of enhancing Ndfip1 to control T cell responses? Increasing Ndfip1 activity could limit cytokine production in macrophages, where it has been shown to function in mouse BMDMs to degrade Tak1 and downregulate NFκB signaling [108]. Whether Ndfip1 regulates
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Protection of DNA is a cancer preventive mechanism both oxid
2020-07-27
Protection of DNA is a cancer preventive mechanism; both oxidative and alkylating damage to colonocytes are known effects of dietary carcinogens. Concerning the DNA protection experiments, two different DNA damaging agents, an oxidant (H2O2) and alkylating (MMS) agent, were used. Hydrogen peroxide i
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br Optimization of the Use of Alkylating
2020-07-27
Optimization of the Use of Alkylating Agents and Platinum Derivatives Concluding Remarks Owing to their broad anticancer spectrum, alkylating agents and platinum derivatives are key in the management of solid tumors. Still, they suffer from acute systemic toxicity, suboptimal treatment schedul
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The nature and role of the prosthetic group As
2020-07-27
The nature and role of the prosthetic group — As mentioned above, Δ1-KSTDs can utilize either phenazine methosulfate or 2,6-dichlorophenol-indophenol as the external electron acceptor. Moreover, the enzyme is strongly inhibited by acriflavin [29,50]. Since these properties have also been observed fo
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In this context cysteine proteases have been investigated in
2020-07-27
In this context, cysteine proteases have been investigated in drug discovery for Chagas disease and HAT. Molecular biology, immunology, pharmacology and medicinal chemistry studies have been conducted to reveal the functions of these enzymes and to validate them for drug discovery purposes (Steverdi
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Keeping in mind the proposed role of CICs
2020-07-27
Keeping in mind the proposed role of CICs in tumor growth and drug resistance [[23], [24], [25]], we focused mainly on factors related to CICs. Mo-treated colonospheres and tumors contained significantly less ALDH1 protein. ALDH1 is regarded as a CSC marker that belongs to a family of cytosolic (and
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Our study demonstrated that atipamezole strongly inhibits th
2020-07-27
Our study demonstrated that atipamezole strongly inhibits the seven-major human CYP isoforms including CYP2C9 (diclofenac 4′-hydroxylation) in HLM, as well as in DLM and RLM. No IC50 shift toward left side was observed indicating the inhibitory effect was in a reversible manner. On the other hand, t
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