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

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-09, Vol.23 (18), p.5049-5052
Main Authors: Pathuri, Gopal, Hedrick, Andria F., Awasthi, Vibhudutta, Ihnat, Michael A., Gali, Hariprasad
Format: Article
Language:English
Subjects:
Aminopeptidase N (APN)
angiogenesis
Animals
biomarkers
CD13
CD13 Antigens - analysis
CD13 Antigens - biosynthesis
CD13 Antigens - metabolism
cell invasion
Cell Line, Tumor
chelating agents
chemistry
computed tomography
fibrosarcoma
Fibrosarcoma - metabolism
Humans
image analysis
Imaging
membrane alanyl aminopeptidase
metastasis
Mice
Mice, Inbred Strains
Mice, Nude
Molecular Imaging - methods
Molecular Structure
N3S chelator
Neoplasms, Experimental - metabolism
Oligopeptides - chemistry
Probestin
SPECT
Tc-99m
Technetium - chemistry
Tomography, Emission-Computed, Single-Photon
Tumor angiogenesis
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Summary: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 99mTc-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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.07.046