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Tumor Biology

Abstract 4205: Targeting a variety of cancers with NOTA-derivatized pH (low) insertion peptide (pHLIP) complexes with 64Cu and 18F: What cancers are targetable

Dustin W. Demoin, Kimberly J. Edwards, Linden C. Wyatt, Mirkka Sarparanta, Jacob Pourat, Oleg A. Andreev, Yana K. Reshetnyak, Nerissa Viola-Villegas and Jason S. Lewis
Dustin W. Demoin
Memorial Sloan Kettering Cancer Center, New York, NY;
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Kimberly J. Edwards
Memorial Sloan Kettering Cancer Center, New York, NY;
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Linden C. Wyatt
University of Rhode Island, Kingston, RI;
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Mirkka Sarparanta
Memorial Sloan Kettering Cancer Center, New York, NY;
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Jacob Pourat
Memorial Sloan Kettering Cancer Center, New York, NY;
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Oleg A. Andreev
University of Rhode Island, Kingston, RI;
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Yana K. Reshetnyak
University of Rhode Island, Kingston, RI;
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Nerissa Viola-Villegas
Karmanos Cancer Institute, Detroit, MI.
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Jason S. Lewis
Memorial Sloan Kettering Cancer Center, New York, NY;
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DOI: 10.1158/1538-7445.AM2016-4205 Published July 2016
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Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA

Abstract

Introduction: Although heterogeneous, the extracellular tumor environment is generally marked by decreased pH relative to nontumor tissues due to cancer cell metabolism. Using a pH-sensitive peptide to deliver diagnostic PET isotopes can provide clinicians with improved diagnostic tools for cancer-specific imaging and an alternative to receptor-based cancer targeting. pH (low) Insertion Peptides (pHLIPs) have previously been shown to target cancerous tissues and are able to deliver PET metals to the cancer site utilizing a NOTA-based chelator.

Methods: The thiol-containing cysteine moiety on the pHLIP peptide sequence was conjugated to the NOTA chelator. The NOTA-derivatized peptides were labeled with 64CuCl2 in 100 mM NH4OAc (pH 5) solution; the [18F]-fluoride was reacted with AlCl3 before forming the [18F]-AlF-NOTA-pHLIP complexes in NH4OAc buffered reaction mixtures (pH ∼ 4.1). After purification and formulation, the radiolabeled peptides were injected intravenously into 4T1 breast, PC-3 prostate, LNCaP prostate, or B16-F10 melanoma tumor-bearing mice.

Results: The 4T1 tumor-bearing mice showed significant uptake > 10%ID/g by 4 h p.i. and continued to show increased uptake of the 64Cu-NOTA-cysVar3 over 20 h. Tumors were visible in the 4T1 tumor-bearing mice as early as 2 h, but had the greatest tumor-to-background ratios at 24 h. Initial studies with B16-F10 tumor-bearing mice showed > 9%ID/g uptake in the tumor by 4 h p.i. with slight increase of 64Cu-NOTA-cysVar3 uptake over 24 h. Due to the placement of the melanoma tumors away from internal organs, tumors were visible by 1 h p.i. Additionally, the size of the melanoma tumors did not affect the%ID/g of radiotracer uptake.

Conclusions: Our studies indicate that the NOTA-cys(pHLIP), specifically NOTA-cysVar3, radiolabeled with 64Cu or 18F is a viable imaging tool for detecting highly metabolic tumors in preclinical mouse models.

Funding: NIH F32 CA186721 (D.W.D.), NIH R01 CA138468 (J.S.L.), NIH MSKCC Center Grant (P30-CA08748).

Citation Format: Dustin W. Demoin, Kimberly J. Edwards, Linden C. Wyatt, Mirkka Sarparanta, Jacob Pourat, Oleg A. Andreev, Yana K. Reshetnyak, Nerissa Viola-Villegas, Jason S. Lewis. Targeting a variety of cancers with NOTA-derivatized pH (low) insertion peptide (pHLIP) complexes with 64Cu and 18F: What cancers are targetable. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 4205.

  • ©2016 American Association for Cancer Research.
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Cancer Research: 76 (14 Supplement)
July 2016
Volume 76, Issue 14 Supplement
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Abstract 4205: Targeting a variety of cancers with NOTA-derivatized pH (low) insertion peptide (pHLIP) complexes with 64Cu and 18F: What cancers are targetable
Dustin W. Demoin, Kimberly J. Edwards, Linden C. Wyatt, Mirkka Sarparanta, Jacob Pourat, Oleg A. Andreev, Yana K. Reshetnyak, Nerissa Viola-Villegas and Jason S. Lewis
Cancer Res July 15 2016 (76) (14 Supplement) 4205; DOI: 10.1158/1538-7445.AM2016-4205

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Abstract 4205: Targeting a variety of cancers with NOTA-derivatized pH (low) insertion peptide (pHLIP) complexes with 64Cu and 18F: What cancers are targetable
Dustin W. Demoin, Kimberly J. Edwards, Linden C. Wyatt, Mirkka Sarparanta, Jacob Pourat, Oleg A. Andreev, Yana K. Reshetnyak, Nerissa Viola-Villegas and Jason S. Lewis
Cancer Res July 15 2016 (76) (14 Supplement) 4205; DOI: 10.1158/1538-7445.AM2016-4205
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