articleScientia PharmaceuticaJan 22, 2025GOLD OA

Targeting c-MYC G-Quadruplexes for Cancer Treatment with Small Molecules

Virginia Commonwealth University · Institute of Medical Sciences · +2 more institutions

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Abstract

Novel therapies are required due to the rising cancer burden. Conventional chemotherapeutics tend to be particularly toxic, but there is a promising alternative for oncogenes, such as c-MYC. Often overexpressed in many cancer types, the potential c-MYC oncogene seems essential to the development of cancer. Targeting c-MYC protein directly was limited, but these DNA structures composed of guanine-rich sequences suppress c-MYC transcription. This review discusses recent advances in developing small compounds that selectively bind to and stabilize c-MYC G-quadruplexes (G4). These molecules have also shown promise for the inhibition of c-MYC signaling and inhibition of tumor growth, suggesting that G-quadruplex…

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