The c-MYC NHE III(1): function and regulation.
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) III(1) region of the c-MYC promoter has 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 on what is known about the formation of a G-quadruplex in the NHE III(1) region of the c-MYC promoter, as well as on 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.
González
Verónica
V
University of Arizona, Tucson, 85721, USA.
Hurley
Laurence H
LH
D000818:Animals; D054856:G-Quadruplexes / Q000187:drug effects; D005786:Gene Expression Regulation; D006801:Humans; D011401:Promoter Regions, Genetic / Q000187:drug effects / Q000502:physiology*; D016271:Proto-Oncogene Proteins c-myc / Q000235:genetics* / Q000502:physiology; D014157:Transcription Factors / Q000502:physiology
D016271:Proto-Oncogene Proteins c-myc; D014157:Transcription Factors