Department of Radiology, School of Medicine, University of Colorado Denver, Aurora, Colorado; and
Department of Biochemistry, University of Missouri-Columbia, and Harry S. Truman Veterans' Hospital, Columbia, Missouri.
J Nucl Med. 2021 Mar;62(3):313-318. doi: 10.2967/jnumed.120.243840. Epub 2020 Dec 4.
Melanocortin-1 receptor (MC1R) and very late antigen-4 (VLA-4, integrin αβ) 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.
黑素皮质素-1 受体 (MC1R) 和非常晚期抗原-4 (VLA-4，整合素 αβ) 是开发用于黑色素瘤成像和治疗的肽放射性药物的 2 个有吸引力的分子靶标。MC1R 和 VLA-4 靶向肽和肽缀合的康奈尔原点 (C' 点) 可以作为载体，将诊断和治疗放射性核素靶向黑色素瘤细胞进行成像和治疗。本文综述了 MC1R 和 VLA-4 靶向放射性标记肽和肽缀合的 C' 点在黑色素瘤成像和治疗中的研究进展。这些新型肽放射性药物的有前途的临床前和临床结果为未来临床转化为受体靶向黑色素瘤成像和放射性核素治疗提供了乐观的前景。
