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BSA was the most efficient compound in reducing inhibition of amplification, due to its binding efficiency.
B2, the most efficient compound, caused obvious DNA damage at 1 μM.
The 3,9-dihydroxy derivative is the most efficient compound of this series toward CDK1/cyclin B and CDK5/p25.
Furthermore, Pd-BENSpm was the most efficient compound regarding induction of DNA damage and decrease in colony formation in soft agar.
To this purpose, we evaluated the effect of methyl- β-cyclodextrin (CD), the most efficient compound used to induce cholesterol depletion from plasma membrane thus disrupting caveolae/lipid rafts [ 22] on VEGFR-2 distribution in the plasma membrane and on VEGF/VEGFR-2 interaction.
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The most efficient compounds displayed inhibition of viability against HUVEC cells in the micromolar range, as observed with TAE-226, which was designed by Novartis Pharma AG.
No single motif has emerged as a universal AO annealing site for redirection of dystrophin pre-mRNA processing, although the general trend is that the most efficient compounds are directed at motifs in the first half of the target exon.
In silico docking suggests a unique mode of binding of the most efficient compounds to the β1 catalytic site (PA activity) in relation to the chemical nature of C1 substituents.
We report substantially different levels of exon skipping induced in normal and dystrophic human myogenic cell lines and propose that animal models or artificial assay systems useful in initial studies may be of limited relevance in designing the most efficient compounds to induce targeted skipping of human dystrophin exons for therapeutic outcomes.
Additionally, in vivo evaluation of the sedative effects of these heterocyclic derivatives showed that 1a and the novel structurally-related analogue 1e were the most efficient compounds to impair the locomotor activity in mice at the dose of 10 μmol/kg.
From the results, it is observed that compounds 3d, 3e, 3f and 3i with electron donating substituents were the most efficient compounds in the FRAP assay (Fig. 1).
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