Evaluation of the Human Melanoma Targeting Properties of Radiolabeled α-Melanocyte Stimulating Hormone Peptide Analogues

2003 ◽  
Vol 14 (6) ◽  
pp. 1177-1184 ◽  
Author(s):  
Yubin Miao ◽  
Donna Whitener ◽  
Weiwei Feng ◽  
Nellie K. Owen ◽  
Jianqing Chen ◽  
...  
Keyword(s):  
Human Melanoma ◽  
Melanocyte Stimulating Hormone ◽  
Peptide Analogues ◽  
Stimulating Hormone

Degradation of alpha-melanocyte stimulating hormone (alpha-MSH) by CALLA/endopeptidase 24. 11 expressed by human melanoma cells in culture

1990 ◽  
Vol 46 (6) ◽  
pp. 1124-1130 ◽  
Author(s):  
Monique Deschodt-Lanckman ◽  
Yves Vanneste ◽  
Béatrice Loir ◽  
Alain Michel ◽  
Anita Libert ◽  
...  
Keyword(s):  
Melanoma Cells ◽  
Human Melanoma ◽  
Melanocyte Stimulating Hormone ◽  
Cells In Culture ◽  
Human Melanoma Cells ◽  
Stimulating Hormone

Alpha-Melanocyte-Stimulating Hormone Immunoreactivity in Human Melanoma Metastases Extracts

1989 ◽  
Vol 2 (6) ◽  
pp. 519-523 ◽  
Author(s):  
G. GHANEM ◽  
J. VERSTEGEN ◽  
A. LIBERT ◽  
R. ARNOULD ◽  
F. LEJEUNE
Keyword(s):  
Human Melanoma ◽  
Melanocyte Stimulating Hormone ◽  
Melanoma Metastases ◽  
Stimulating Hormone

scholarly journals 111In-Labeled Lactam Bridge-Cyclized α-Melanocyte Stimulating Hormone Peptide Analogues for Melanoma Imaging

2008 ◽  
Vol 19 (2) ◽  
pp. 539-547 ◽  
Author(s):  
Yubin Miao ◽  
Fabio Gallazzi ◽  
Haixun Guo ◽  
Thomas P. Quinn
Keyword(s):  
Melanocyte Stimulating Hormone ◽  
Lactam Bridge ◽  
Peptide Analogues ◽  
Stimulating Hormone

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

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Chengcheng Zhang ◽  
Zhengxing Zhang ◽  
Helen Merkens ◽  
Jutta Zeisler ◽  
Nadine Colpo ◽  
...  
Keyword(s):  
Human Melanoma ◽  
Image Contrast ◽  
Post Injection ◽  
Tumor Uptake ◽  
Isotope Exchange Reaction ◽  
Melanocyte Stimulating Hormone ◽  
Molar Activity ◽  
Human Melanoma Xenograft ◽  
Melanoma Xenograft ◽  
Stimulating Hormone

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 xenografts. The MC1R density on the SK-MEL-1 cell line was determined to be 972 ± 154 receptors/cell (n = 4) via saturation assays. Using [18F]CCZ01064, moderate tumor uptake (3.05 ± 0.47%ID/g) and image contrast were observed at 2 h post-injection. Molar activity was determined to play a key role. CCZ01096 with two AmBF3 motifs showed comparable sub-nanomolar binding affinity to MC1R and much higher molar activity. This resulted in improved tumor uptake (6.46 ± 1.42%ID/g) and image contrast (tumor-to-blood and tumor-to-muscle ratios were 30.6 ± 5.7 and 85.7 ± 11.3, respectively) at 2 h post-injection. [18F]CCZ01096 represents a promising αMSH-based μPET imaging agent for human melanoma and warrants further investigation for potential clinical translation.

Novel α-Melanocyte Stimulating Hormone Peptide Analogues with High Candidacidal Activity

2003 ◽  
Vol 46 (5) ◽  
pp. 850-855 ◽  
Author(s):  
Paolo Grieco ◽  
Claudia Rossi ◽  
Gualtiero Colombo ◽  
Stefano Gatti ◽  
Ettore Novellino ◽  
...  
Keyword(s):  
Melanocyte Stimulating Hormone ◽  
Peptide Analogues ◽  
Stimulating Hormone
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