4.6 Review Book Chapter

The c-MYC NHE III1: Function and Regulation

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DOI: 10.1146/annurev.pharmtox.48.113006.094649

关键词

G-quadruplex; nucleolin; CNBP; hnRNP K; superhelicity; NM23-H2

资金

  1. National Institutes of Health [CA122952, CA95060, GM085585]
  2. NATIONAL CANCER INSTITUTE [P50CA095060, R01CA122952] Funding Source: NIH RePORTER
  3. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM085585] Funding Source: NIH RePORTER

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c-MYC is an important regulator of a wide array of cellular processes necessary, for normal cell growth and differentiation, and its dysregulation is one of the hallmarks of many cancers. Consequently, understanding c-MYC transcriptional activation is critical for understanding developmental and cancer biology as well as for the development of new anticancer drugs. The nuclease hypersensitive element (NHE) III1 region of the c-MYC promoter his been shown to be particularly important in regulating c-MYC expression. Specifically, the formation of a G-quadruplex structure appears to promote repression of c-MYC transcription. This review focuses oil whit is known about the formation of a G-quadruplex in the NHE III1 region of the c-MYC promoter, as well as oil those factors that are known to modulate its formation. Last, we discuss the development of small molecules that stabilize or induce the formation of G-quadruplex structures and could potentially be used as anticancer agents.

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