Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Radiolabeled Alpha-Melanocyte Stimulating Hormone Derivatives for Development of Malignant Melanoma Imaging Agents

  • Chaewon Lee (College of Pharmacy and Research Institute of Pharmaceutical Science, Gyeongsang National University) ;
  • Dong-Yeon Kim (College of Pharmacy and Research Institute of Pharmaceutical Science, Gyeongsang National University)
  • Received : 2023.12.06
  • Accepted : 2023.12.15
  • Published : 2023.12.30
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Abstract

Malignant melanoma is a very aggressive metastatic skin cancer with a high mortality rate. Thus, an accurate early diagnosis of metastatic melanoma is the best treatment for patients. The melanocortin-1 receptor (MC1R) is overexpressed in human melanoma cells but exhibits low expression in normal tissues. This characteristic makes it an attractive target for detection of malignant melanoma. Alpha-melanocyte stimulating hormone (α-MSH), one of the endogenous ligands of MC1R, binds to MC1R through its core sequence. However, it is challenging to utilize the native structure of α-MSH, so researchers have found that stabilizing it through cyclization can offer more favorable outcomes in both preclinical and clinical studies. This review introduces the development of radionuclide-labeled α-MSH derivatives that selectively bind to MC1R, a malignant melanoma-specific target. It also explains on the development of cyclized α-MSH derivatives and the results of biological evaluations related to renal uptake.

Keywords

Acknowledgement

이 성과는 정부(과학기술정보통신부)의 재원으로 한국연구재단의 지원(NRF-2020R1C1C1012379 및 (NRF-2021M2E7A-3085685)과 산업통상자원부 및 산업기술평가관리원(KEIT) 연구비 지원(20016670)에 의한 연구이며, 다른 상업적 이해관계는 없음.

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