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Characterization and solubilization of pyrrole-imidazole polyamide aggregates. PDF available through Get Fulltext Research

Hargrove, Amanda E Raskatov, Jevgenij A Meier, Jordan L Montgomery, David C Dervan, Peter B

Published in Journal of medicinal chemistry

To optimize the biological activity of pyrrole-imidazole polyamide DNA-binding molecules, we characterized the aggregation propensity of these compounds through dynamic light scattering and fractional solubility analysis. Nearly all studied polyamides were found to form measurable particles 50-500 nm in size under biologically relevant conditions, ...

Tumor xenograft uptake of a pyrrole-imidazole (Py-Im) polyamide varies as a function of cell line grafted. PDF available through Get Fulltext Research

Raskatov, Jevgenij A Szablowski, Jerzy O Dervan, Peter B

Published in Journal of medicinal chemistry

Subcutaneous xenografts represent a popular approach to evaluate efficacy of prospective molecular therapeutics in vivo. In the present study, the C-14 labeled radioactive pyrrole-imidazole (Py-Im) polyamide 1, targeted to the 5'-WGWWCW-3' DNA sequence, was evaluated with regard to its uptake properties in subcutaneous xenografts, derived from the ...

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