In vivo evaluation of 99mTc/188Re-labeled linear alpha-melanocyte stimulating hormone analogs for specific melanoma targeting
In vivo evaluation of 99mTc/188Re-labeled linear alpha-melanocyte stimulating hormone analogs for specific melanoma targeting
复制标题
DOI：
10.1016/s0969-8051(99)00032-3
复制
发表时间：
1999-08-01
影响因子：
3.1
通讯作者：
Quinn, TP
中科院分区：
文献类型：
--
作者：
Chen, JQ;Giblin, MF;Quinn, TP
在携带黑色素瘤的小鼠中检查放射性标记的α-黑素细胞刺激激素（α-MSH）类似物，以确定肽长度、结构和放射性金属螯合化学对肿瘤靶向和体内生物分布的影响。线性 α-MSH 类似物 [Nle(4)、D-Phe(7)]α-MSH (NDPMSH) 和 [D-Phe(7)]α-MSH5-10 (DPMSH) 通过添加四氟苯基巯基-乙酰甘氨酰甘氨酰-γ-氨基 (MAG(2)) 或四肽，用 Tc-99m 和 Re-188 进行放射性标记Ac-Cys-Gly-Cys-Gly (CGCG) 螯合部分。 I-125-Tyr(2)-NDPMSH 通过直接碘化 Tyr(2) 残基获得。注射后 30 分钟，Tc-99m 标记的 CGCG- 和 MAG(2)-NDPMSH 类似物的肿瘤摄取分别为 6.52 +/- 1.11 %ID/g 和 4.17 +/- 1.34 %ID/g，导致肿瘤与血液的摄取比显着高于 I-125-NDPMSH 或较短的 α-MSH 类似物， Tc-99m-CGCG DPMSH。放射性标记功效与体内肿瘤摄取的结合凸显了 Tc-99m-CGCG-NDPMSH 作为黑色素瘤成像剂的潜力。 NUCL MED BIOL 26;6:687-693, 1999。(C) 1999 Elsevier Science Inc. 保留所有权利。
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 [Nle(4), D-Phe(7)]alpha-MSH (NDPMSH) and [D-Phe(7)]alpha-MSH5-10 (DPMSH) were radiolabeled with Tc-99m and Re-188 via the addition of tetrafluorophenyl mercapto-acetylglycylglycyl-gamma-aminob (MAG(2)) or tetrapeptide Ac-Cys-Gly-Cys-Gly (CGCG) chelation moieties. I-125-Tyr(2)-NDPMSH was obtained by direct iodination of the Tyr(2) residue. Tumor uptake of Tc-99m-labeled CGCG- and MAG(2)-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 I-125-NDPMSH or a shorter alpha-MSH analog, Tc-99m-CGCG DPMSH. The combination of radiolabeling efficacy and in vivo tumor uptake highlights the potential of Tc-99m-CGCG-NDPMSH as a melanoma imaging agent. NUCL MED BIOL 26;6:687-693, 1999. (C) 1999 Elsevier Science Inc. All rights reserved.