G-Quadruplexes in c-MYC Promoter as Targets for Cancer Therapy

Cancer is a societal burden demanding innovative approaches. A major problem with the conventional chemotherapeutic agents is their strong toxicity and other side effects due to their poor selectivity. Uncontrolled proliferation of cancer cells is due to mutations, deletions, or amplifications in genes (oncogenes) encoding for proteins that regulate cell growth and division, such as transcription factors, for example, c-MYC. The direct targeting of the c-MYC protein has been attempted but so far unsuccessfully, as it lacks a definite binding site for the modulators. Meanwhile, another approach has been explored since the discovery that G-quadruplex secondary DNA structures formed in the guanine-rich sequences of the c-MYC promoter region can downregulate the transcription of this oncogene. Here, we will overview the major achievements made in the last decades towards the discovery of a new class of anticancer drugs targeting G-quadruplexes in the c-MYC promoter of cancer cells.

Automated summary

Cancer is a societal burden that requires innovative approaches due to the toxic side effects and poor selectivity of conventional chemotherapeutic agents. Uncontrolled proliferation of cancer cells is caused by mutations, deletions, or amplifications in genes encoding for proteins that regulate cell growth and division, such as c-MYC. Directly targeting the c-MYC protein has been unsuccessful, but the exploration of G-quadruplex structures in the c-MYC promoter region has shown promise in downregulating the transcription of this oncogene. In this article, we will overview the significant advancements made in the discovery of a new class of anticancer drugs that target G-quadruplexes in the c-MYC promoter of cancer cells.