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.
Radiotracers for positron emission tomography (PET) targeting tumour-associated carbonic anhydrase isoforms / Burianova, Valeria; Kalinin, Stanislav; Supuran, Claudiu T; Krasavin, Mikhail. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - ELETTRONICO. - 213:(2021), pp. 0-0. [10.1016/j.ejmech.2020.113046]
Radiotracers for positron emission tomography (PET) targeting tumour-associated carbonic anhydrase isoforms
Supuran, Claudiu T;
2021
Abstract
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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