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用于正电子发射断层扫描黑色素瘤成像的具有多个甲基化的选择性环化α-黑素细胞刺激激素衍生物

Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple -Methylations for Melanoma Imaging with Positron Emission Tomography.

作者信息

Zhang Chengcheng, Zhang Zhengxing, Zeisler Jutta, Colpo Nadine, Lin Kuo-Shyan, Bénard François

机构信息

Department of Molecular Oncology, BC Cancer, 675 W 10th Avenue, Vancouver, British Columbia V5Z 1L3, Canada.

Department of Radiology, University of British Columbia, 2775 Laurel Street, Vancouver, British Columbia V5Z 1M9, Canada.

出版信息

ACS Omega. 2020 May 7;5(19):10767-10773. doi: 10.1021/acsomega.0c00310. eCollection 2020 May 19.

DOI:10.1021/acsomega.0c00310
PMID:32455196
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7240809/
Abstract

In this study, we designed and evaluated a novel α-melanocyte-stimulating hormone derivative with four -methylations for melanocortin 1 receptor-targeted melanoma imaging with positron emission tomography (PET). The resulting peptide, DOTA-Pip-Nle-Cyclo[Asp--Me-His-d-Phe--Me-Arg--Me-Trp--Me-Lys]αMSH-NH (CCZ01099), showed high receptor selectivity, greatly improved stability, and rapid internalization. [Ga]Ga-CCZ01099 showed clear tumor visualization and excellent tumor-to-normal tissue contrast with PET imaging in a preclinical melanoma model. Therefore, CCZ01099 is a promising compound for imaging and potentially radioligand therapy for melanoma.

摘要

在本研究中，我们设计并评估了一种具有四个甲基化修饰的新型α-黑素细胞刺激激素衍生物，用于正电子发射断层扫描（PET）靶向黑素皮质素1受体的黑色素瘤成像。所得肽DOTA-Pip-Nle-Cyclo[Asp--Me-His-d-Phe--Me-Arg--Me-Trp--Me-Lys]αMSH-NH（CCZ01099）表现出高受体选择性、显著提高的稳定性和快速内化。[Ga]Ga-CCZ01099在临床前黑色素瘤模型的PET成像中显示出清晰的肿瘤可视化和出色的肿瘤与正常组织对比度。因此，CCZ01099是一种有前景的用于黑色素瘤成像及潜在放射性配体治疗的化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/b60e7d4492b0/ao0c00310_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/506b1058c0fc/ao0c00310_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/3fc026a1afb4/ao0c00310_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/d9017270d0a0/ao0c00310_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/b60e7d4492b0/ao0c00310_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/506b1058c0fc/ao0c00310_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/3fc026a1afb4/ao0c00310_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/d9017270d0a0/ao0c00310_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7240809/b60e7d4492b0/ao0c00310_0004.jpg

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