Vāvere Amy L, Lewis Jason S
Department of Radiology, Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Dalton Trans. 2007 Nov 21(43):4893-902. doi: 10.1039/b705989b. Epub 2007 Sep 25.
Copper(II)-diacetyl-bis(N(4)-methylthiosemicarbazone), Cu-ATSM, labeled with a positron emitting isotope of copper ((60)Cu, (61)Cu, (62)Cu or (64)Cu) has been shown, in vitro and in vivo, to be selective for hypoxic tissue. In silico studies have explored the mechanism of its hypoxia selectivity, and clinical studies with this agent have shown non-invasive imaging data that is predictive of a cancer patients' response to conventional therapy. This Perspective discusses the evolution of Cu-ATSM, how its selectivity can be improved upon, and where this metal-ligand platform could be taken in the future.
铜（II）-二乙酰双（N（4）-甲基硫代半卡巴腙），即Cu-ATSM，用铜的正电子发射同位素（（60）Cu、（61）Cu、（62）Cu或（64）Cu）标记后，已在体外和体内实验中显示对缺氧组织具有选择性。计算机模拟研究探索了其缺氧选择性的机制，并且该药物的临床研究已显示出可预测癌症患者对传统疗法反应的非侵入性成像数据。本观点讨论了Cu-ATSM的发展历程、如何改进其选择性以及该金属-配体平台未来的发展方向。
