Advances in Receptor-Targeted Radiolabeled Peptides for Melanoma Imaging and Therapy

J Nucl Med. 2021 Mar;62(3):313-318. doi: 10.2967/jnumed.120.243840. Epub 2020 Dec 4.

Abstract

Melanocortin-1 receptor (MC1R) and very late antigen-4 (VLA-4, integrin α4β1) are 2 attractive molecular targets for developing peptide radiopharmaceuticals for melanoma imaging and therapy. MC1R- and VLA-4-targeting peptides and peptide-conjugated Cornell prime dots (C' dots) can serve as delivery vehicles to target both diagnostic and therapeutic radionuclides to melanoma cells for imaging and therapy. This review highlights the advances of MC1R- and VLA-4-targeted radiolabeled peptides and peptide-conjugated C' dots for melanoma imaging and therapy. The promising preclinical and clinical results of these new peptide radiopharmaceuticals present an optimistic outlook for clinical translation into receptor-targeting melanoma imaging and radionuclide therapy in the future.

Keywords: Cornell prime dots; melanocortin-1 receptor; melanoma imaging and therapy; peptide radiopharmaceuticals; very late antigen-4.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Humans
  • Isotope Labeling
  • Melanoma / diagnostic imaging*
  • Melanoma / metabolism
  • Melanoma / radiotherapy*
  • Molecular Imaging / methods*
  • Molecular Targeted Therapy*
  • Receptors, Peptide / metabolism*

Substances

  • Receptors, Peptide