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In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography

Harki, Daniel A. and Satyamurthy, Nagichettiar and Stout, David B. and Phelps, Michael E. and Dervan, Peter B. (2008) In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography. Proceedings of the National Academy of Sciences of the United States of America, 105 (35). pp. 13039-13044. ISSN 0027-8424. PMCID PMC2529060. doi:10.1073/pnas.0806308105.

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The biodistribution profiles in mice of two pyrrole-imidazole polyamides were determined by PET. Pyrrole-imidazole polyamides are a class of small molecules that can be programmed to bind a broad repertoire of DNA sequences, disrupt transcription factor-DNA interfaces, and modulate gene expression pathways in cell culture experiments. The 18F-radiolabeled polyamides were prepared by oxime ligation between 4-[18F]-fluorobenzaldehyde and a hydroxylamine moiety at the polyamide C terminus. Small animal PET imaging of radiolabeled polyamides administered to mice revealed distinct differences in the biodistribution of a 5-ring β-linked polyamide versus an 8-ring hairpin, which exhibited better overall bioavailability. In vivo imaging of pyrrole-imidazole polyamides by PET is a minimum first step toward the translation of polyamide-based gene regulation from cell culture to small animal studies.

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Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 2008 by The National Academy of Sciences of the USA. Contributed by Peter B. Dervan, June 30, 2008 (sent for review April 8, 2008) We thank the staffs of the Biomedical Cyclotron Facility and the Crump Preclinical Imaging Center at the University of California, Los Angeles for helpful discussions and support, and Dr. Mona Shahgholi (California Institute of Technology) for assistance with UPLC-MS analysis. This work was supported by National Institutes of Health Grants GM27681, R01-EB001943, and R24 CA 92865; National Science Foundation Chemistry Research Instrumentation and Facilities Program Grant CHE-0541745; and the Department of Energy Cooperative Agreement DE-FC03-02ER63420. D.A.H. thanks the Friedreich's Ataxia Research Alliance and the California Tobacco-Related Disease Research Program (16FT-0055) for postdoctoral fellowships. Author Contributions: D.A.H., N.S., D.B.S., M.E.P., and P.B.D. designed research; D.A.H., N.S., and D.B.S. performed research; D.A.H., N.S., D.B.S., M.E.P., and P.B.D. analyzed data; and D.A.H., N.S., D.B.S., M.E.P., and P.B.D. wrote the paper. The authors declare no conflict of interest. This article contains supporting information online at
Funding AgencyGrant Number
NIHR24 CA 92865
Department of Energy (DOE)DE-FC03-02ER63420
Friedreich’s Ataxia Research AllianceUNSPECIFIED
California Tobacco-Related Disease Research Program16FT-0055
Subject Keywords:biodistribution; fluorine-18; oxime; radiosynthesis
Issue or Number:35
PubMed Central ID:PMC2529060
Record Number:CaltechAUTHORS:HARpnas08
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Official Citation:Daniel A. Harki, Nagichettiar Satyamurthy, David B. Stout, Michael E. Phelps, and Peter B. Dervan In vivo imaging of pyrrole-imidazole polyamides with positron emission tomography PNAS 2008 105 (35) 13039-13044; published ahead of print August 27, 2008, doi:10.1073/pnas.0806308105
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:11859
Deposited By: Archive Administrator
Deposited On:07 Oct 2008 22:58
Last Modified:08 Nov 2021 22:22

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