Lys¹(α,γ-叶酸)Lys³(¹⁷⁷Lu-DOTA)-蛙皮素(1 - 14)作为一种潜在的乳腺癌诊疗放射性药物的合成与评价
Synthesis and evaluation of Lys¹(α,γ-Folate)Lys³(¹⁷⁷Lu-DOTA)-Bombesin(1-14) as a potential theranostic radiopharmaceutical for breast cancer.
作者信息
Aranda-Lara Liliana, Ferro-Flores Guillermina, Azorín-Vega Erika, Ramírez Flor de María, Jiménez-Mancilla Nallely, Ocampo-García Blanca, Santos-Cuevas Clara, Isaac-Olivé Keila
机构信息
Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico; Facultad de Medicina, Universidad Autónoma del Estado de México, Toluca 50180, Mexico.
Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
出版信息
Appl Radiat Isot. 2016 Jan;107:214-219. doi: 10.1016/j.apradiso.2015.10.030. Epub 2015 Oct 28.
The aim of this work was to synthesize Lys(1)(α,γ-Folate)-Lys(3)((177)Lu-DOTA)-Bombesin (1-14) ((177)Lu-Folate-BN), as well as to assess its potential for molecular imaging and targeted radiotherapy of breast tumors expressing folate receptors (FR) and gastrin-releasing peptide receptors (GRPR). Radiation absorbed doses of (177)Lu-Folate-BN (74 MBq, i.v.) estimated in athymic mice with T47D-induced breast tumors (positive to FR and GRPR), showed tumor doses of 23.9±2.1 Gy. T47D-tumors were clearly visible (Micro-SPECT/CT images). (177)Lu-Folate-BN demonstrated properties suitable as a theranostic radiopharmaceutical.
本研究的目的是合成赖氨酸(1)(α,γ-叶酸)-赖氨酸(3)((177)镥-二乙基三胺五乙酸)-蛙皮素(1 - 14) ((177)镥-叶酸-蛙皮素)，并评估其在表达叶酸受体(FR)和胃泌素释放肽受体(GRPR)的乳腺肿瘤分子成像和靶向放射治疗中的潜力。在患有T47D诱导的乳腺肿瘤(FR和GRPR呈阳性)的无胸腺小鼠中估计的(177)镥-叶酸-蛙皮素(74 MBq，静脉注射)的辐射吸收剂量显示肿瘤剂量为23.9±2.1 Gy。T47D肿瘤清晰可见(Micro-SPECT/CT图像)。(177)镥-叶酸-蛙皮素表现出适合作为治疗诊断放射性药物的特性。
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