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Targeting Carbonic Anhydrase IX in Tumor Imaging and Theranostic Cancer Therapy

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The Carbonic Anhydrases: Current and Emerging Therapeutic Targets

Part of the book series: Progress in Drug Research ((PDR,volume 75))

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Abstract

Carbonic anhydrase IX (CA-IX) is an endogenous marker for hypoxia and is regulated by the von Hippel-Lindau/hypoxia-inducible factor (VHL/HIF) oxygen-sensing pathway. CA-IX is overexpressed in many solid malignancies where aberrant vasculature and limited perfusion create low oxygen niches within the tumor microenvironment. Dysregulation of the VHL/HIF signaling pathway can lead to constitutive expression of CA-IX—a phenotype associated with clear cell renal cell carcinomas (ccRCCs). As a cell-surface metalloenzyme, CA-IX works in tandem with other proteins to regulate intracellular pH in response to hypoxia-induced metabolism. In recent years, there has been evidence implicating CA-IX in potentiating cancer invasion and metastasis. Accordingly, the inhibition of CA-IX catalytic activity represents an attractive option for the management of ccRCC and other solid tumors. In this chapter, we discuss the development of CA-IX radiopharmaceuticals and their roles in delineating tumoral CA-IX expression through imaging in preclinical and clinical settings. We will also review agents that have been repositioned as endoradiotherapeutic agents for theranostic application.

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Authors and Affiliations

  1. Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC, V5Z 1L3, Canada

    Joseph Lau, Kuo-Shyan Lin & François Bénard

Authors
  1. Joseph Lau
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  2. Kuo-Shyan Lin
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  3. François Bénard
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Correspondence to François Bénard .

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Editors and Affiliations

  1. LECOM, Erie, PA, USA

    W. Richard Chegwidden

  2. St. George’s, University of London, London, UK

    Nicholas D. Carter

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Lau, J., Lin, KS., Bénard, F. (2021). Targeting Carbonic Anhydrase IX in Tumor Imaging and Theranostic Cancer Therapy. In: Chegwidden, W.R., Carter, N.D. (eds) The Carbonic Anhydrases: Current and Emerging Therapeutic Targets. Progress in Drug Research, vol 75. Springer, Cham. https://doi.org/10.1007/978-3-030-79511-5_12

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