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Bioorg Med Chem Lett. 2014 Jan 1;24(1):195-8. doi: 10.1016/j.bmcl.2013.11.042. Epub 2013 Nov 23.

Linker modification reduced the renal uptake of technetium-99m-labeled Arg-Ala-Asp-conjugated alpha-melanocyte stimulating hormone peptide.

Author information

  • 12502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
  • 22502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA; Cancer Research and Treatment Center, University of New Mexico, Albuquerque, NM 87131, USA; Department of Dermatology, University of New Mexico, Albuquerque, NM 87131, USA. Electronic address: ymiao@salud.unm.edu.

Abstract

The purpose of this study was to examine the biodistribution of (99m)Tc-RAD-Arg-(Arg(11))CCMSH in B16/F1 melanoma-bearing C57 mice to determine whether the replacement of the Lys linker with an Arg linker could decrease the renal uptake of (99m)Tc-RAD-Arg-(Arg(11))CCMSH. (99m)Tc-RAD-Arg-(Arg(11))CCMSH exhibited rapid and high tumor uptake (17.98±4.96% ID/g at 2h post-injection) in B16/F1 melanoma-bearing C57 mice. As compared to (99m)Tc-RAD-Lys-(Arg(11))CCMSH, the replacement of the Lys linker with an Arg linker dramatically decreased the renal uptake of (99m)Tc-RAD-Arg-(Arg(11))CCMSH by 68%, 62%, 73% and 64% at 0.5, 2, 4 and 24h post-injection, respectively. Flank B16/F1 melanoma lesions were clearly imaged at 2h post-injection using (99m)Tc-RAD-Arg-(Arg(11))CCMSH as an imaging probe.

Copyright © 2013 Elsevier Ltd. All rights reserved.

KEYWORDS:

Alpha-melanocyte stimulating hormone peptide; Melanocortin-1 receptor; Melanoma imaging; Renal uptake

PMID:
24316121
[PubMed - indexed for MEDLINE]
PMCID:
PMC3889140
Free PMC Article
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