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

Raskatov, Jevgenij A. and Puckett, James W. and Dervan, Peter B. (2014) A C-14 labeled Py–Im polyamide localizes to a subcutaneous prostate cancer tumor. Bioorganic and Medicinal Chemistry, 22 (16). pp. 4371-4375. ISSN 0968-0896. PMCID PMC4134956.

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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.

Item Type:Article
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URLURL TypeDescription CentralArticle
Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2014 Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license ( 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).
Funding AgencyGrant Number
Alexander von Humboldt FoundationUNSPECIFIED
Subject Keywords:Accumulation; C-14 radiolabeling; Chemotherapy; DNA binding; Small molecule
Issue or Number:16
PubMed Central ID:PMC4134956
Record Number:CaltechAUTHORS:20140505-092742935
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Official Citation:Jevgenij A. Raskatov, James W. Puckett, Peter B. Dervan, A C-14 labeled Py–Im polyamide localizes to a subcutaneous prostate cancer tumor, Bioorganic & Medicinal Chemistry, Volume 22, Issue 16, 15 August 2014, Pages 4371-4375, ISSN 0968-0896, (
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:45485
Deposited By: Tony Diaz
Deposited On:05 May 2014 17:52
Last Modified:03 Oct 2019 06:31

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