Journal of Enzyme Inhibition and Medicinal Chemistry · 2018 · 19 citations · 52 references
MedicineCancer BiologyOncologyMetastasisTumor MicroenvironmentTumor ProgressionCancer Cell SignalingCancer MetabolismCancer ProgressionHypoxia AdaptationMalignant NeoplasmsTumor Microenvironment ModulationCarbonic Anhydrase InhibitorsCarbonic Anhydrase TargetsHif-1 SignalingHypoxic MicroenvironmentSelective Cancer TherapyTherapeutic Target IdentificationTumor Microenvironment HypoxiaTumor Microenvironment Regulation
The hypoxic tumour microenvironment of solid tumours represents an important starting point for modulating progression and metastatic spread. Carbonic anhydrase IX (CAIX) is a known HIF-1α-dependent key player in maintaining cell pH conditions under hypoxia. We show that CAIX is strongly expressed in esophageal carcinoma tissues. We hypothesize that a moderate CAIX expression facilitates metastases and thereby worsens prognosis. Selective inhibition of CAIX by specific CAIX inhibitors and a CAIX knockdown effectively inhibit proliferation and migration in vitro. In the orthotopic esophageal carcinoma model, the humanized HER2 antibody trastuzumab down-regulates CAIX, possibly through CAIX's linkage with HER2 in the hypoxic microenvironment. Our results show CAIX to be an essential part of the tumour microenvironment and a possible master regulator of tumour progression. This makes CAIX a highly effective and feasible therapeutic target for selective cancer treatment.
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