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

[Image: see text] In this study, we designed and evaluated a novel α-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-Nle(4)-Cyclo[Asp(5)-N-Me-His(6)-d-Phe...

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Autores principales: Zhang, Chengcheng, Zhang, Zhengxing, Zeisler, Jutta, Colpo, Nadine, Lin, Kuo-Shyan, Bénard, François
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7240809/
https://www.ncbi.nlm.nih.gov/pubmed/32455196
http://dx.doi.org/10.1021/acsomega.0c00310
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author Zhang, Chengcheng
Zhang, Zhengxing
Zeisler, Jutta
Colpo, Nadine
Lin, Kuo-Shyan
Bénard, François
author_facet Zhang, Chengcheng
Zhang, Zhengxing
Zeisler, Jutta
Colpo, Nadine
Lin, Kuo-Shyan
Bénard, François
author_sort Zhang, Chengcheng
collection PubMed
description [Image: see text] In this study, we designed and evaluated a novel α-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-Nle(4)-Cyclo[Asp(5)-N-Me-His(6)-d-Phe(7)-N-Me-Arg(8)-N-Me-Trp(9)-N-Me-Lys(10)]αMSH(4-10)-NH(2) (CCZ01099), showed high receptor selectivity, greatly improved stability, and rapid internalization. [(68)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.
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spelling pubmed-72408092020-05-22 Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography Zhang, Chengcheng Zhang, Zhengxing Zeisler, Jutta Colpo, Nadine Lin, Kuo-Shyan Bénard, François ACS Omega [Image: see text] In this study, we designed and evaluated a novel α-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-Nle(4)-Cyclo[Asp(5)-N-Me-His(6)-d-Phe(7)-N-Me-Arg(8)-N-Me-Trp(9)-N-Me-Lys(10)]αMSH(4-10)-NH(2) (CCZ01099), showed high receptor selectivity, greatly improved stability, and rapid internalization. [(68)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. American Chemical Society 2020-05-07 /pmc/articles/PMC7240809/ /pubmed/32455196 http://dx.doi.org/10.1021/acsomega.0c00310 Text en Copyright © 2020 American Chemical Society This is an open access article published under a Creative Commons Non-Commercial No Derivative Works (CC-BY-NC-ND) Attribution License (http://pubs.acs.org/page/policy/authorchoice_ccbyncnd_termsofuse.html) , which permits copying and redistribution of the article, and creation of adaptations, all for non-commercial purposes.
spellingShingle Zhang, Chengcheng
Zhang, Zhengxing
Zeisler, Jutta
Colpo, Nadine
Lin, Kuo-Shyan
Bénard, François
Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography
title Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography
title_full Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography
title_fullStr Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography
title_full_unstemmed Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography
title_short Selective Cyclized α-Melanocyte-Stimulating Hormone Derivative with Multiple N-Methylations for Melanoma Imaging with Positron Emission Tomography
title_sort selective cyclized α-melanocyte-stimulating hormone derivative with multiple n-methylations for melanoma imaging with positron emission tomography
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7240809/
https://www.ncbi.nlm.nih.gov/pubmed/32455196
http://dx.doi.org/10.1021/acsomega.0c00310
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