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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Raskatov, JA; Hargrove, AE; So, AY; Dervan, PB

Published Date

  • May 2012

Published In

Volume / Issue

  • 134 / 18

Start / End Page

  • 7995 - 7999

PubMed ID

  • 22509786

Pubmed Central ID

  • PMC3349014

Electronic International Standard Serial Number (EISSN)

  • 1520-5126

International Standard Serial Number (ISSN)

  • 0002-7863

Digital Object Identifier (DOI)

  • 10.1021/ja302588v


  • eng