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Positively charged templates for labeling internalizing antibodies: comparison of N-succinimidyl 5-iodo-3-pyridinecarboxylate and the D-amino acid peptide KRYRR.

Publication ,  Journal Article
Foulon, CF; Welsh, PC; Bigner, DD; Zalutsky, MR
Published in: Nucl Med Biol
October 2001

Receptor-mediated internalization of monoclonal antibodies (mAbs), such as those specific for the epidermal growth factor receptor variant III (EGFRvIII), can lead to rapid loss of radioactivity from the target cell. In the current study, the anti-EGFRvIII mAb L8A4 was radioiodinated using two methods -N-succinimidyl 5-iodo-3-pyridinecarboxylate (SIPC) and via a D-amino acid peptide LysArgTyrArgArg (D-KRYRR). Paired-label internalization assays performed on EGFRvIII-expressing U87DeltaEGFR cells in vitro demonstrated that labeling L8A4 using D-KRYRR resulted in significantly higher retention of radioiodine in the intracellular compartment. In athymic mice with D256 human glioma xenografts, tumor uptake was similar for both labeling methods through 24 hr. However, an up to fourfold higher tumor retention was observed for mAb labeled with the D-amino acid peptide at later time points. Radiation absorbed dose calculations based on these biodistribution data indicated that L8A4 labeled using D-KRYRR exhibited better tumor-to-normal-organ radiation dose ratios, suggesting that this labeling method may be of particular value for labeling internalizing mAbs.

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Published In

Nucl Med Biol

DOI

ISSN

0969-8051

Publication Date

October 2001

Volume

28

Issue

7

Start / End Page

769 / 777

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Succinimides
  • Radiopharmaceuticals
  • Radiometry
  • Oligopeptides
  • Nuclear Medicine & Medical Imaging
  • Nicotinic Acids
  • Neoplasm Transplantation
  • Mice, Nude
 

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Foulon, C. F., Welsh, P. C., Bigner, D. D., & Zalutsky, M. R. (2001). Positively charged templates for labeling internalizing antibodies: comparison of N-succinimidyl 5-iodo-3-pyridinecarboxylate and the D-amino acid peptide KRYRR. Nucl Med Biol, 28(7), 769–777. https://doi.org/10.1016/s0969-8051(01)00239-6
Foulon, C. F., P. C. Welsh, D. D. Bigner, and M. R. Zalutsky. “Positively charged templates for labeling internalizing antibodies: comparison of N-succinimidyl 5-iodo-3-pyridinecarboxylate and the D-amino acid peptide KRYRR.Nucl Med Biol 28, no. 7 (October 2001): 769–77. https://doi.org/10.1016/s0969-8051(01)00239-6.
Foulon, C. F., et al. “Positively charged templates for labeling internalizing antibodies: comparison of N-succinimidyl 5-iodo-3-pyridinecarboxylate and the D-amino acid peptide KRYRR.Nucl Med Biol, vol. 28, no. 7, Oct. 2001, pp. 769–77. Pubmed, doi:10.1016/s0969-8051(01)00239-6.
Journal cover image

Published In

Nucl Med Biol

DOI

ISSN

0969-8051

Publication Date

October 2001

Volume

28

Issue

7

Start / End Page

769 / 777

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Succinimides
  • Radiopharmaceuticals
  • Radiometry
  • Oligopeptides
  • Nuclear Medicine & Medical Imaging
  • Nicotinic Acids
  • Neoplasm Transplantation
  • Mice, Nude