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Pharmacokinetics of Py-Im polyamides depend on architecture: cyclic versus linear.

ABSTRACT: The pharmacokinetic properties of three pyrrole-imidazole (Py-Im) polyamides of similar size and Py-Im content but different shape were studied in the mouse. Remarkably, hairpin and cyclic oligomers programmed for the same DNA sequence 5'-WGGWWW-3' displayed distinct pharmacokinetic properties. Furthermore, the hairpin 1 and cycle 2 exhibited vastly different animal toxicities. These data provide a foundation for design of DNA binding Py-Im polyamides to be tested in vivo.

SUBMITTER: Raskatov JA 

PROVIDER: S-EPMC3349014 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature

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Pharmacokinetics of Py-Im polyamides depend on architecture: cyclic versus linear.

Raskatov Jevgenij A JA   Hargrove Amanda E AE   So Alex Y AY   Dervan Peter B PB  

Journal of the American Chemical Society 20120424 18

The pharmacokinetic properties of three pyrrole-imidazole (Py-Im) polyamides of similar size and Py-Im content but different shape were studied in the mouse. Remarkably, hairpin and cyclic oligomers programmed for the same DNA sequence 5'-WGGWWW-3' displayed distinct pharmacokinetic properties. Furthermore, the hairpin 1 and cycle 2 exhibited vastly different animal toxicities. These data provide a foundation for design of DNA binding Py-Im polyamides to be tested in vivo. ...[more]

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