Versant Medical Physics and Radiation Safety, Richland , Washington 99354 , United States.
Mol Pharm. 2019 Apr 1;16(4):1694-1702. doi: 10.1021/acs.molpharmaceut.9b00025. Epub 2019 Feb 25.
The purpose of this study is to examine the melanocortin-1 receptor (MC1R) targeting and specificity of Pb-DOTA-GGNle-CycMSH in melanoma cells and tumors to facilitate its potential therapeutic application when labeled with Pb. The MC1R-specific targeting and imaging properties of Pb-DOTA-GGNle-CycMSH were determined on B16/F1 and B16/F10 murine melanoma cells and in B16/F1 flank melanoma-, B16/F10 flank melanoma-, and B16/F10 pulmonary metastatic melanoma-bearing C57 mice. Pb-DOTA-GGNle-CycMSH displayed MC1R-specific binding on B16/F1 and B16/F10 melanoma cells and tumors. B16/F1 flank melanoma, B16/F10 flank melanoma, and B16/F10 pulmonary metastatic melanoma lesions could be clearly imaged by single photon emission computed tomography (SPECT) using Pb-DOTA-GGNle-CycMSH as an imaging probe. The favorable melanoma targeting and imaging properties highlighted the potential of Pb-DOTA-GGNle-CycMSH as a MC1R-targeting melanoma imaging probe and warranted the evaluation of Pb-DOTA-GGNle-CycMSH for melanoma therapy in future studies.
本研究旨在研究黑素皮质素-1 受体（MC1R）在黑色素瘤细胞和肿瘤中的靶向性和特异性，以便在标记 Pb 后促进其潜在的治疗应用。在 B16/F1 和 B16/F10 小鼠黑色素瘤细胞以及 B16/F1 侧翼黑色素瘤、B16/F10 侧翼黑色素瘤和 B16/F10 肺转移性黑色素瘤荷瘤 C57 小鼠中，确定了 Pb-DOTA-GGNle-CycMSH 的 MC1R 特异性靶向和成像特性。Pb-DOTA-GGNle-CycMSH 在 B16/F1 和 B16/F10 黑色素瘤细胞和肿瘤上显示出 MC1R 特异性结合。使用 Pb-DOTA-GGNle-CycMSH 作为成像探针，可通过单光子发射计算机断层扫描（SPECT）清楚地对 B16/F1 侧翼黑色素瘤、B16/F10 侧翼黑色素瘤和 B16/F10 肺转移性黑色素瘤病变进行成像。良好的黑色素瘤靶向性和成像特性突出了 Pb-DOTA-GGNle-CycMSH 作为 MC1R 靶向黑色素瘤成像探针的潜力，值得在未来的研究中评估 Pb-DOTA-GGNle-CycMSH 用于黑色素瘤治疗。
