三唑附加剂（TAAG）：一种用于制备碘基分子成像和放射治疗剂的新型合成子。
Triazole Appending Agent (TAAG): A New Synthon for Preparing Iodine-Based Molecular Imaging and Radiotherapy Agents.
作者信息
Darwish Alla, Blacker Megan, Janzen Nancy, Rathmann Stephanie M, Czorny Shannon, Hillier Shawn M, Joyal John L, Babich John W, Valliant John F
机构信息
Department of Chemistry and Chemical Biology, McMaster University , 1280 Main Street West, Hamilton, Ontario L8S 4L8, Canada.
Centre for Probe Development and Commercialization, McMaster University , 1280 Main Street West Hamilton, Ontario L8S 4K1, Canada.
出版信息
ACS Med Chem Lett. 2012 Feb 18;3(4):313-6. doi: 10.1021/ml300003v. eCollection 2012 Apr 12.
A new prosthetic group referred to as the triazole appending agent (TAAG) was developed as a means to prepare targeted radioiodine-based molecular imaging and therapy agents. Tributyltin-TAAG and the fluorous analogue were synthesized in high yield using simple click chemistry and the products labeled in greater than 95% RCY with (123)I. A TAAG derivative of an inhibitor of prostate-specific membrane antigen was prepared and radiolabeled with (123)I in 85% yield where biodistribution studies in LNCap prostate cancer tumor models showed rapid clearance of the agent from nontarget tissues and tumor accumulation of 20% injected dose g(-1) at 1 h. The results presented demonstrate that the TAAG group promotes minimal nonspecific binding and that labeled conjugates can achieve high tumor uptake and exquisite target-to-nontarget ratios.
一种被称为三唑附加剂（TAAG）的新型辅基被开发出来，作为制备基于放射性碘的靶向分子成像和治疗剂的一种手段。使用简单的点击化学方法高产率地合成了三丁基锡-TAAG及其氟代类似物，产物用（123）I标记，放射化学产率大于95%。制备了前列腺特异性膜抗原抑制剂的TAAG衍生物，并用（123）I进行放射性标记，产率为85%，在LNCap前列腺癌肿瘤模型中的生物分布研究表明，该试剂能从非靶组织快速清除，在1小时时肿瘤摄取量为注射剂量的20% g-1。所呈现的结果表明，TAAG基团促进的非特异性结合最小，且标记的缀合物可实现高肿瘤摄取和优异的靶非靶比。
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