Evaluation of 99mTc-probestin for imaging APN expressing tumors by SPECT.

Abstract

Aminopeptidase N (APN) is known to play important roles in tumor angiogenesis, tumor cell invasion, and metastasis. Thus, APN is an attractive biomarker for imaging tumor angiogenesis. Here we report results obtained from biodistribution and single photon emission computed tomography (SPECT) imaging studies of a technetium-99m labeled probestin (a potent APN inhibitor) conjugate containing a tripeptide, Asp-DAP-Cys (DAP=2,3-diaminopropionic acid), chelator and a 8-amino-3,6-dioxaoctanoic acid (PEG2) linker conducted in nude mice xenografted with HT-1080 human fibrosarcoma tumors (APN-positive tumors). These results collectively demonstrate that (99m)Tc-probestin uptake by tumors and other APN expressing tissues in vivo is specific and validate the use of probestin as a vector for targeting APN in vivo.

• Authors: Gopal Pathuri, Andria F Hedrick, Vibhudutta Awasthi, Michael A Ihnat, Hariprasad Gali
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 18 Pg. 5049-52 (Sep 15 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 23937983 (Publication Type: Evaluation Study, Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Ltd. All rights reserved.

Chemical References

• Oligopeptides
• probestin
• Technetium
• CD13 Antigens

Topics

• Animals
• CD13 Antigens (analysis, biosynthesis, metabolism)
• Cell Line, Tumor
• Fibrosarcoma (metabolism)
• Humans
• Mice
• Mice, Inbred Strains
• Mice, Nude
• Molecular Imaging (methods)
• Molecular Structure
• Neoplasms, Experimental (metabolism)
• Oligopeptides (chemistry)
• Technetium (chemistry)
• Tomography, Emission-Computed, Single-Photon