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ZEB antagonists are small molecule inhibitors developed by the Leuven Centre for Drug Design and Discovery (CD3) that target the Zinc finger E-box-binding homeobox (ZEB) family of transcription factors, specifically ZEB1 and ZEB2. These proteins are master regulators of the epithelial-mesenchymal transition (EMT), a cellular process that allows epithelial cancer cells to acquire mesenchymal properties, thereby increasing their motility, invasiveness, and resistance to apoptosis. By inhibiting ZEB activity, these compounds aim to reverse the EMT process, which can suppress metastatic spread, overcome resistance to chemotherapy and immunotherapy, and target cancer stem cell populations. The program is currently in the preclinical stage of development for the treatment of various solid cancers.
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