用丙氨酸取代甘氨酸增强了[99mTc]标记的 Arg-Ala-Asp 缀合的α-黑色素细胞刺激激素肽的黑色素瘤摄取。
Substitution of Gly with Ala enhanced the melanoma uptake of technetium-99m-labeled Arg-Ala-Asp-conjugated alpha-melanocyte stimulating hormone peptide.
机构信息
College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1541-5. doi: 10.1016/j.bmcl.2012.01.003. Epub 2012 Jan 10.
Abstract
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.
摘要
本研究旨在确定 (99m)Tc-RAD-Lys-(Arg(11))CCMSH 在 B16/F1 黑色素瘤荷瘤 C57 小鼠中的黑色素瘤靶向特性，并与我们之前报道的 (99m)Tc-RGD-Lys-(Arg(11))CCMSH 进行比较。(99m)Tc-RAD-Lys-(Arg(11))CCMSH 在 B16/F1 黑色素瘤荷瘤 C57 小鼠中表现出快速和高肿瘤摄取（注射后 2 小时为 19.91±4.02% ID/g）。(99m)Tc-RAD-Lys-(Arg(11))CCMSH 的肿瘤摄取在 0.5、2 和 4 小时分别是 (99m)Tc-RGD-Lys-(Arg(11))CCMSH 的肿瘤摄取的 1.51、1.34 和 1.43 倍。使用 (99m)Tc-RAD-Lys-(Arg(11))CCMSH 作为成像探针，在注射后 2 小时可清晰地对侧翼 B16/F1 黑色素瘤病变进行成像。与 (99m)Tc-RGD-Lys-(Arg(11))CCMSH 相比，甘氨酸被丙氨酸取代显著增强了 (99m)Tc-RAD-Lys-(Arg(11))CCMSH 在 B16/F1 黑色素瘤荷瘤 C57 小鼠中的黑色素瘤摄取，为设计用于黑色素瘤靶向的 α-MSH 肽提供了新的见解。
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