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Published August 15, 2014 | Published + Supplemental Material
Journal Article Open

A C-14 labeled Py–Im polyamide localizes to a subcutaneous prostate cancer tumor

Abstract

In an effort to quantitate Py–Im polyamide concentrations in vivo, we synthesized the C-14 radioactively labeled compounds 1–3, and investigated their tumor localization in a subcutaneous xenograft model of prostate cancer (LNCaP). Tumor concentrations were compared with representative host tissues, and exhibited a certain degree of preferential localization to the xenograft. Compound accumulation upon repeated administration was measured. Py–Im polyamide 1 was found to accumulate in LNCaP tumors at concentrations similar to the IC_(50) value for this compound in cell culture experiments.

Additional Information

© 2014 Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/3.0/). Received 14 February 2014; Accepted 6 April 2014. JAR is grateful to the Alexander von Humboldt foundation for the award of a Feodor Lynen postdoctoral fellowship. Professor Bogdan Olenyuk is gratefully acknowledged for helpful discussion. We are indebted to Dr. Janet Baer, Dr. Karen Lencioni and Dr. Haick Issaian for their help with technical aspects of experimental design. We are grateful for support by the National Institutes of Health (GM51747 and GM27681).

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Published - 1-s2.0-S0968089614002545-main.pdf

Supplemental Material - mmc1.pdf

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