Department of Neuroimaging and Interventional Radiology (NI & IR), National Institute of Mental Health and Neurosciences (NIMHANS), Bengaluru 560 029, India.
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India.
Bioorg Chem. 2023 Apr;133:106399. doi: 10.1016/j.bioorg.2023.106399. Epub 2023 Jan 30.
Positron emission tomography (PET) and fluorescent imaging play a pivotal role in medical diagnosis, biomedical oncologic research, and drug development process, which include identification of target location, target engagement, but also prove on mechanism of action or pharmacokinetics of new drug candidates. PET estimates physiological changes at the molecular level using specific radiotracers containing a short-lived positron emitting radionuclide such as fluorine-18 or carbon-11, whereas fluorescent imaging techniques use fluorescent probes labeled with suitable drug candidates for detection at the molecular level. The human carbonic anhydrase (hCA) isoforms IX and XII are overexpressed in hypoxic cancer cells, promoting tumor growth by regulating extra/intracellular pH, ferroptosis, and metabolism, being recognized as promising targets for anticancer theranostic agents. In this review, we have focused on PET radiotracers as well as fluorescent probes for diagnosis and treatment of tumors expressing hCA IX and hCA XII.
正电子发射断层扫描（PET）和荧光成像是医学诊断、生物医学肿瘤学研究和药物开发过程中的关键技术，包括确定靶点位置、靶点结合，还可以证明新候选药物的作用机制或药代动力学。PET 使用含有短寿命正电子发射放射性核素（如氟-18 或碳-11）的特定放射性示踪剂来估计分子水平的生理变化，而荧光成像技术则使用标记有合适候选药物的荧光探针在分子水平进行检测。人类碳酸酐酶（hCA）同工型 IX 和 XII 在缺氧癌细胞中过度表达，通过调节细胞外/内 pH 值、铁死亡和代谢来促进肿瘤生长，被认为是用于癌症诊断和治疗的有前途的药物。在本综述中，我们重点介绍了用于诊断和治疗表达 hCA IX 和 hCA XII 的肿瘤的 PET 放射性示踪剂和荧光探针。
