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Gallium-67-Labeled Lactam Bridge-Cyclized Alpha-MSH Peptides with Enhanced Melanoma Uptake and Reduced Renal Uptake
| Content Provider | Scilit |
|---|---|
| Author | Guo, Haixun Gallazzi, Fabio Miao, Yubin |
| Copyright Year | 2012 |
| Abstract | The purpose of this study was to examine the melanoma targeting and pharmacokinetic properties of$ $^{67}$Ga-DOTA-GGNle-CycMSH_{hex}$ ${^{67}$Ga-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraacetic $acid-Gly-Gly-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH_{2}$} and$ $^{67}$Ga-NOTA-GGNle-CycMSH_{hex}$ ${^{67}$Ga-1,4,7-triazacyclononane-1,4,7-triacetic $acid-Gly-Gly-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH_{2}$} and compare with$ ^{67}$Ga-DOTA-GlyGlu-CycMSH ${^{67}$Ga-DOTA-Gly-Glu-c[Lys-Nle-Glu-His-DPhe-Arg-Trp-Gly-Arg-Pro-Val-Asp]} we previously reported. $DOTA-GGNle-CycMSH_{hex}$ and $NOTA-GGNle-CycMSH_{hex}$ were synthesized using fluorenylmethyloxy carbonyl (Fmoc) chemistry. The melanocortin-1 (MC1) receptor binding affinity of $NOTA-GGNle-CycMSH_{hex}$ was determined in B16/F1 melanoma cells and compared with $DOTA-GGNle-CycMSH_{hex}$. The melanoma targeting and pharmacokinetic properties of$ $^{67}$Ga-NOTA-GGNle-CycMSH_{hex}$ and$ $^{67}$Ga-DOTA-GGNle-CycMSH_{hex}$ were determined in B16/F1 melanoma-bearing C57 mice. $NOTA-GGNle-CycMSH_{hex}$ and $DOTA-GGNle-CycMSH_{hex}$ displayed comparable MC1 receptor binding affinities (1.6 vs 2.1 nM) in B16/F1 melanoma cells. Both$ $^{67}$Ga-NOTA-GGNle-CycMSH_{hex}$ and$ $^{67}$Ga-DOTA-GGNle-CycMSH_{hex}$ exhibited dramatically enhanced melanoma uptake and reduced renal uptake than$ ^{67}$Ga-DOTA-GlyGlu-CycMSH in B16/F1 melanoma-bearing C57 mice. Furthermore,$ $^{67}$Ga-NOTA-GGNle-CycMSH_{hex}$ exhibited more favorable radiolabeling conditions (>85% radiolabeling yields started at 37 °C), as well as higher tumor/kidney uptake ratios than$ $^{67}$Ga-DOTA-GGNle-CycMSH_{hex}$ at 0.5, 2, and 24 h postinjection. High melanoma uptake coupled with low renal uptake highlighted the potential of$ $^{67}$Ga-NOTA-GGNle-CycMSH_{hex}$ for melanoma imaging and therapy. |
| Related Links | http://europepmc.org/articles/pmc3440555?pdf=render https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3440555/pdf |
| Ending Page | 1348 |
| Page Count | 8 |
| Starting Page | 1341 |
| ISSN | 10431802 |
| e-ISSN | 15204812 |
| DOI | 10.1021/bc300191z |
| Journal | Bioconjugate Chemistry |
| Issue Number | 6 |
| Volume Number | 23 |
| Language | English |
| Publisher | American Chemical Society (ACS) |
| Publisher Date | 2012-06-20 |
| Access Restriction | Open |
| Subject Keyword | Journal: Bioconjugate Chemistry Medicinal Chemistry Alpha-melanocyte Stimulating Hormone Lactam Bridge-cyclized Peptide Melanoma Targeting |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Pharmacology Bioengineering Biomedical Engineering Biotechnology Pharmaceutical Science |
