¹⁸F-Labeled Cyclized α-Melanocyte-Stimulating Hormone Derivatives for Imaging Human Melanoma Xenograft with Positron Emission Tomography.

ABSTRACT: Since metastatic melanoma is deadly, early diagnosis thereof is crucial for managing the disease. We recently developed α-melanocyte-stimulating hormone (αMSH) derivatives, [⁶⁸Ga]Ga-CCZ01048 and [¹⁸F]CCZ01064, that target the melanocortin 1 receptor (MC1R) for mouse melanoma imaging. In this study, we aim to evaluate [¹⁸F]CCZ01064 as well as a novel dual-ammoniomethyl-trifluoroborate (AmBF₃) derivative, [¹⁸F]CCZ01096, for targeting human melanoma xenograft using μPET imaging. The peptides were synthesized on solid phase using Fmoc chemistry. Radiolabeling was achieved in a one-step ¹⁸F-¹⁹F isotope-exchange reaction. μPET imaging and biodistribution studies were performed in NSG mice bearing SK-MEL-1 melanoma xenog

SUBMITTER: Zhang C 

PROVIDER: S-EPMC6753210 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature