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

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2 Scopus citations

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.

Original languageEnglish
Article number113046
JournalEuropean Journal of Medicinal Chemistry
DOIs
StateAccepted/In press - 2020

Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Keywords

  • Hypoxic tumour markers
  • Membrane-bound carbonic anhydrase isoforms
  • Monoclonal antibodies
  • Positron emission tomography
  • Positron-emitting radionuclides
  • Small-molecule inhibitors

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