Radiotracers for positron emission tomography (PET) targeting tumour-associated carbonic anhydrase isoforms

被引:17
作者
Burianova, Valeria [1 ]
Kalinin, Stanislav [1 ]
Supuran, Claudiu T. [2 ]
Krasavin, Mikhail [1 ]
机构
[1] St Petersburg State Univ, Inst Chem, St Petersburg, Russia
[2] Univ Florence, Neurofarba Dept, Sect Pharmaceut Sci, Florence, Italy
关键词
Hypoxic tumour markers; Positron emission tomography; Membrane-bound carbonic anhydrase isoforms; Positron-emitting radionuclides; Monoclonal antibodies; Small-molecule inhibitors;
D O I
10.1016/j.ejmech.2020.113046
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2020 Elsevier Masson SAS. All rights reserved.
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页数:18
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