镓-PSMA-BCH 的合成及前列腺癌成像的临床前评价。
Synthesis and preclinical evaluation of Ga-PSMA-BCH for prostate cancer imaging.
机构信息
Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China.
Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China.
出版信息
Bioorg Med Chem Lett. 2019 Apr 1;29(7):933-937. doi: 10.1016/j.bmcl.2019.01.013. Epub 2019 Jan 17.
Prostate specific membrane antigen (PSMA) is a promising target for the diagnosis and therapy of prostate cancer. In this report, a NOTA-conjugated precursor, NOTA-PSMA (also named PSMA-BCH), was synthesized by peptide synthesizer with the chemical purity over 95%. Ga-PSMA-BCH was obtained by radiolabeling NOTA-PSMA with GaCl with >99% radiochemical purity and 59-74 GBq/μmol specific activity. In vitro and in vivo study of Ga-PSMA-BCH showed high stability, high uptake in PSMA-expressing cells and tumor, fast clearance and low non-target uptake. 22Rv1 tumors were clearly observed in micro-PET images of and showed good retention. Compared with Ga-PSMA-617, Ga-PSMA-BCH showed comparable tumor uptake and tumor-background ratios. Indicating Ga-PSMA-BCH is a promising candidate for prostate cancer imaging and worthy of further clinical investigations.
前列腺特异性膜抗原（PSMA）是前列腺癌诊断和治疗有前途的靶点。在本报告中，通过肽合成仪合成了一种 NOTA 缀合前体 NOTA-PSMA（也称为 PSMA-BCH），其化学纯度超过 95%。用 GaCl3 对 NOTA-PSMA 进行放射性标记，得到 Ga-PSMA-BCH，其放射化学纯度>99%，比活度为 59-74GBq/μmol。Ga-PSMA-BCH 的体外和体内研究表明其具有高稳定性、在 PSMA 表达细胞和肿瘤中摄取率高、清除速度快、非靶摄取率低。22Rv1 肿瘤在 micro-PET 图像中清晰可见，并具有良好的保留性。与 Ga-PSMA-617 相比，Ga-PSMA-BCH 显示出可比的肿瘤摄取和肿瘤-背景比。表明 Ga-PSMA-BCH 是一种有前途的前列腺癌成像候选药物，值得进一步临床研究。
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