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Melanotan-I

Afamelanotide, MT-I, [Nle4-D-Phe7]-α-MSH, Scenesse, CUV-1647

Quick Stats
Studies 225
Trials 100
Overview Studies Clinical Trials
1999 pubmed

In vivo evaluation of 99mTc/188Re-labeled linear alpha-melanocyte stimulating hormone analogs for specific melanoma targeting.

Chen. J J; Giblin. M F MF; Wang. N N; Jurisson. S S SS; Quinn. T P TP

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Key Findings

  • Peptide length and chelator type strongly influence how much of the radioactive peptide ends up in melanoma tumors.
  • The 99mTc‑CGCG‑NDPMSH construct showed the highest tumor uptake and best tumor‑to‑blood ratio among the tested compounds.
  • Radiolabeling chemistry (choice of metal and chelator) is crucial for creating effective melanoma imaging agents.

Practical Outcomes

  • This work is mainly relevant for developing medical imaging tools for melanoma and does not provide actionable protocols for personal health optimization or performance enhancement. Biohackers are unlikely to apply these findings directly.

Summary

Scientists tested different versions of a skin‑pigment hormone peptide attached to radioactive tags in mice with melanoma to see which version best highlights tumors for imaging. The version with a small CGCG chelator and technetium‑99m gave the strongest tumor signal.

Abstract

Radiolabeled alpha-melanocyte stimulating hormone (alpha-MSH) analogs were examined in melanoma-bearing mice to determine the effects of peptide length, structure, and radiometal chelation chemistry on tumor targeting and in vivo biodistribution. The linear alpha-MSH analogs [Nle4,D-Phe7]alpha-MSH (NDPMSH) and [D-Phe7]alpha-MSH(5-10) (DPMSH) were radiolabeled with 99mTc and 188Re via the addition of tetrafluorophenyl mercapto-acetylglycylglycyl-gamma-aminobutyrate (MAG2) or tetrapeptide Ac-Cys-Gly-Cys-Gly (CGCG) chelation moieties. 125I-Tyr2-NDPMSH was obtained by direct iodination of the Tyr2 residue. Tumor uptake of 99mTc-labeled CGCG- and MAG2-NDPMSH analogs at 30 min postinjection were 6.52 +/- 1.11 %ID/g and 4.17 +/- 1.34 %ID/g, respectively, resulting in a significantly higher tumor-to-blood uptake ratio than that of 125I-NDPMSH or a shorter alpha-MSH analog, 99mTc-CGCG-DPMSH. The combination of radiolabeling efficacy and in vivo tumor uptake highlights the potential of 99mTc-CGCG-NDPMSH as a melanoma imaging agent.

Study Information

Provider

pubmed

Year

1999

DOI

10.1016/s0969-8051(99)00032-3