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PeerJ. 2017 Nov 23;5:e4068. doi: 10.7717/peerj.4068. eCollection 2017.

An update on anticancer drug development and delivery targeting carbonic anhydrase IX.

Author information

Department of Biothermodynamics and Drug Design, Institute of Biotechnology, Vilnius University, Vilnius, Lithuania.
Faculty of Medicine and Life sciences, University of Tampere, Tampere, Finland.
Fimlab Ltd, Tampere, Finland.
Contributed equally


The expression of carbonic anhydrase (CA) IX is up-regulated in many types of solid tumors in humans under hypoxic and acidic microenvironment. Inhibition of CA IX enzymatic activity with selective inhibitors, antibodies or labeled probes has been shown to reverse the acidic environment of solid tumors and reduce the tumor growth establishing the significant role of CA IX in tumorigenesis. Thus, the development of potent antitumor drugs targeting CA IX with minimal toxic effects is important for the target-specific tumor therapy. Recently, several promising antitumor agents against CA IX have been developed to treat certain types of cancers in combination with radiation and chemotherapy. Here we review the inhibition of CA IX by small molecule compounds and monoclonal antibodies. The methods of enzymatic assays, biophysical methods, animal models including zebrafish and Xenopus oocytes, and techniques of diagnostic imaging to detect hypoxic tumors using CA IX-targeted conjugates are discussed with the aim to overview the recent progress related to novel therapeutic agents that target CA IX in hypoxic tumors.


CA IX antitumor agents; CA IX monoclonal antibodies; Carbonic anhydrase IX; Conjugated probes; Drug development; Hypoxic tumors

Conflict of interest statement

Daumantas Matulis declares that he has patents and patent applications for CA inhibiting compounds. Ashok Aspatwar and Seppo Parkkila are currently employed by Fimlab Ltd. Other authors confirm that this article content has no conflicts of interest.

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