One attractive approach to anticancer therapy is repression of expression of vascular endothelial growth factor (VEGF) gene, which is a potent target for prevention of tumor growth. To achieve this, artificial transcription factors (ATF) designed for VEGF gene regulation were fused to cell-penetrating peptides (CPPs). We demonstrated ATFs fused to CPPs, designated CPP-ATFs or designed regulatory proteins (DRPs), could penetrate into mammalian cells and transiently repress expression of a reporter gene, which was under control of the VEGF promoter/5'-UTR. We discuss gene-regulatory properties of CPP-ATFs in detail.
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