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


ABSTRACT: In this study, we designed and evaluated a novel ?-melanocyte-stimulating hormone derivative with four N-methylations for melanocortin 1 receptor-targeted melanoma imaging with positron emission tomography (PET). The resulting peptide, DOTA-Pip-Nle4-Cyclo[Asp5-N-Me-His6-d-Phe7-N-Me-Arg8-N-Me-Trp9-N-Me-Lys10]?MSH4-10-NH2 (CCZ01099), showed high receptor selectivity, greatly improved stability, and rapid internalization. [68Ga]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.

SUBMITTER: Zhang C 

PROVIDER: S-EPMC7240809 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple <i>N</i>-Methylations for Melanoma Imaging with Positron Emission Tomography.

Zhang Chengcheng C   Zhang Zhengxing Z   Zeisler Jutta J   Colpo Nadine N   Lin Kuo-Shyan KS   Bénard François F  

ACS omega 20200507 19


In this study, we designed and evaluated a novel α-melanocyte-stimulating hormone derivative with four <i>N</i>-methylations for melanocortin 1 receptor-targeted melanoma imaging with positron emission tomography (PET). The resulting peptide, DOTA-Pip-Nle<sup>4</sup>-Cyclo[Asp<sup>5</sup>-<i>N</i>-Me-His<sup>6</sup>-d-Phe<sup>7</sup>-<i>N</i>-Me-Arg<sup>8</sup>-<i>N</i>-Me-Trp<sup>9</sup>-<i>N</i>-Me-Lys<sup>10</sup>]αMSH<sub>4-10</sub>-NH<sub>2</sub> (CCZ01099), showed high receptor selectivity  ...[more]

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