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Literature DB >> 22509786

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

Jevgenij A Raskatov¹, Amanda E Hargrove, Alex Y So, Peter B Dervan.

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.

Entities: Chemical Disease Gene Species

Mesh：

Substances：
Imidazoles
Nylons
Pyrroles

Year: 2012 PMID： 22509786 PMCID： PMC3349014 DOI： 10.1021/ja302588v

Source DB: PubMed Journal: J Am Chem Soc ISSN： 0002-7863 Impact factor: 15.419

27 in total

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Journal: Tetrahedron Date: 2007-07-02 Impact factor: 2.457

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Authors: Nicholas G Nickols; Peter B Dervan
Journal: Proc Natl Acad Sci U S A Date: 2007-06-12 Impact factor: 11.205

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Authors: J M Belitsky; D H Nguyen; N R Wurtz; Peter B Dervan
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9. Modulating hypoxia-inducible transcription by disrupting the HIF-1-DNA interface.

Authors: Nicholas G Nickols; Claire S Jacobs; Michelle E Farkas; Peter B Dervan
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Authors: Daniel A Harki; Nagichettiar Satyamurthy; David B Stout; Michael E Phelps; Peter B Dervan
Journal: Proc Natl Acad Sci U S A Date: 2008-08-27 Impact factor: 11.205

18 in total

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2. Correlation of local effects of DNA sequence and position of β-alanine inserts with polyamide-DNA complex binding affinities and kinetics.

Authors: Shuo Wang; Rupesh Nanjunda; Karl Aston; James K Bashkin; W David Wilson
Journal: Biochemistry Date: 2012-11-28 Impact factor: 3.162

3. Gene expression changes in a tumor xenograft by a pyrrole-imidazole polyamide.

Authors: Jevgenij A Raskatov; Nicholas G Nickols; Amanda E Hargrove; Georgi K Marinov; Barbara Wold; Peter B Dervan
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4. A C-14 labeled Py-Im polyamide localizes to a subcutaneous prostate cancer tumor.

Authors: Jevgenij A Raskatov; James W Puckett; Peter B Dervan
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5. Androgen receptor antagonism by divalent ethisterone conjugates in castrate-resistant prostate cancer cells.

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6. Binding studies of a large antiviral polyamide to a natural HPV sequence.

Authors: Gaofei He; Elena Vasilieva; George Davis Harris; Kevin J Koeller; James K Bashkin; Cynthia M Dupureur
Journal: Biochimie Date: 2014-02-26 Impact factor: 4.079

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