Substitution of Gly with Ala enhanced the melanoma uptake of technetium-99m-labeled Arg-Ala-Asp-conjugated alpha-melanocyte stimulating hormone peptide.
The purpose of this study was to determine the melanoma targeting property of (99m)Tc-RAD-Lys-(Arg(11))CCMSH in B16/F1 melanoma-bearing C57 mice and compare with (99m)Tc-RGD-Lys-(Arg(11))CCMSH we previously reported. (99m)Tc-RAD-Lys-(Arg(11))CCMSH exhibited rapid and high tumor uptake (19.91±4.02% ID/g at 2h post-injection) in B16/F1 melanoma-bearing C57 mice. The tumor uptake of (99m)Tc-RAD-Lys-(Arg(11))CCMSH was 1.51, 1.34 and 1.43 times the tumor uptake of (99m)Tc-RGD-Lys-(Arg(11))CCMSH at 0.5, 2 and 4h post-injection, respectively. Flank B16/F1 melanoma lesions were clearly imaged at 2h post-injection using (99m)Tc-RAD-Lys-(Arg(11))CCMSH as an imaging probe. The substitution of Gly with Ala significantly enhanced the melanoma uptake of (99m)Tc-RAD-Lys-(Arg(11))CCMSH compared to (99m)Tc-RGD-Lys-(Arg(11))CCMSH in B16/F1 melanoma-bearing C57 mice, providing a new insight into the design of α-MSH peptides for melanoma targeting.
College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
Jianquan
J
Yang
Yubin
Y
Miao
D000818:Animals; D001667:Binding, Competitive; D045744:Cell Line, Tumor; D005998:Glycine / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008545:Melanoma / Q000175:diagnosis* / Q000000981:diagnostic imaging / Q000378:metabolism* / Q000473:pathology; D051379:Mice; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry; D010446:Peptide Fragments / Q000737:chemistry*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry*; D013667:Technetium / Q000737:chemistry*; D000521:alpha-MSH / Q000737:chemistry*
D009842:Oligopeptides; D010446:Peptide Fragments; D019275:Radiopharmaceuticals; D000521:alpha-MSH; D013667:Technetium; C047981:arginyl-glycyl-aspartic acid; D005998:Glycine