Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russia.
Neurofarba Department, Section of Pharmaceutical Sciences, University of Florence, Florence, Italy.
Eur J Med Chem. 2021 Mar 5;213:113046. doi: 10.1016/j.ejmech.2020.113046. Epub 2020 Nov 25.
The tumour-associated, cell membrane-bound isoforms IX and XII of human carbonic anhydrase (CA, EC 4.2.1.1) are overexpressed in cancer cells contributing to the hypoxic tumour pH/metabolism regulating machinery and as thus, can serve as markers of malignant neoplastic tissue. Inhibitors of CAs can be employed both for the treatment of hypoxic tumours and in the design of radiotracers for positron emission tomography and imaging of such cancers. The present review provides a comprehensive summary of the progress achieved to-date in the field of developing PET-tracers based on monoclonal antibodies, biomolecules, and small-molecule ligands of CA IX and XII.
肿瘤相关的、细胞膜结合的人碳酸酐酶 (CA,EC 4.2.1.1) 的同工型 IX 和 XII 在癌细胞中过表达,有助于缺氧肿瘤 pH/代谢调节机制,因此可以作为恶性肿瘤组织的标志物。碳酸酐酶抑制剂可用于治疗缺氧肿瘤,并可用于设计正电子发射断层扫描放射性示踪剂和此类癌症的成像。本综述全面总结了目前在开发基于单克隆抗体、生物分子和 CAIX 和 XII 的小分子配体的 PET 示踪剂方面所取得的进展。