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MC1R 及黑色素相关分子探针在黑色素瘤诊治中的应用及其他相关领域

MC1R and melanin-based molecular probes for theranostic of melanoma and beyond.

机构信息

State Key Laboratory of Drug Research, Molecular Imaging Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.

University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing, 100049, China.

出版信息

Acta Pharmacol Sin. 2022 Dec;43(12):3034-3044. doi: 10.1038/s41401-022-00970-y. Epub 2022 Aug 25.

Abstract

Malignant melanoma is accounting for most of skin cancer-associated mortality. The incidence of melanoma increased every year worldwide especially in western countries. Treatment efficiency is highly related to the stage of melanoma. Therefore, accurate staging and restaging play a pivotal role in the management of melanoma patients. Though F-fluorodeoxyglucose (F-FDG) positron-emission tomography (PET) has been widely used in imaging of tumor metastases, novel radioactive probes for specific targeted imaging of both primary and metastasized melanoma are still desired. Melanocortin receptor 1 (MC1R) and melanin are two promising biomarkers specifically for melanoma, and numerous research groups including us have been actively developing a plethora of radioactive probes based on targeting of MC1R or melanin for over two decades. In this review, some of the MC1R-targeted tracers and melanin-associated molecular imaging probes developed in our research and others have been briefly summarized, and it provides a quick glance of melanoma-targeted probe design and may contribute to further developing novel molecular probes for cancer theranostics.

摘要

恶性黑素瘤是导致皮肤癌相关死亡的主要原因。全球范围内,黑素瘤的发病率每年都在上升,尤其是在西方国家。治疗效果与黑素瘤的分期密切相关。因此,准确的分期和再分期在黑素瘤患者的管理中起着关键作用。虽然 F-氟脱氧葡萄糖(F-FDG)正电子发射断层扫描(PET)已广泛应用于肿瘤转移的成像,但仍需要用于原发性和转移性黑素瘤的特定靶向成像的新型放射性探针。黑素皮质素受体 1(MC1R)和黑色素是两种有前途的黑素瘤特异性生物标志物,包括我们在内的许多研究小组在过去二十多年中一直积极开发基于 MC1R 或黑色素靶向的大量放射性探针。在这篇综述中,简要总结了我们研究中开发的一些针对 MC1R 的示踪剂和黑色素相关的分子成像探针,以及其他一些探针,为黑素瘤靶向探针设计提供了快速浏览,并可能有助于进一步开发用于癌症治疗的新型分子探针。

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