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Structure of the biologically relevant G-quadruplex in the c-MYC promoter.

Author information

1
University of Arizona, College of Pharmacy, Tucson, AZ 85721, USA.

Abstract

The nuclease hypersensitivity element III1 (NHE III1) in the c-MYC promoter controls up to 80-90% of the transcriptional activity of this gene. We have demonstrated that the guanine-rich strand of the NHE III1 forms a G-quadruplex consisting of a mixture of four biologically relevant loop isomers that function as a silencer element. NMR studies have shown that these G-quadruplexes are propeller-type parallel structures consisting of three stacked G-tetrads and three double-chain reversal loops. An NMR-derived solution structure for this quadruplex provides insight into the unusual stability of the structure. This structure is a target for small molecule inhibitors of c-MYC gene expression.

PMID:
16901825
DOI:
10.1080/15257770600809913
[Indexed for MEDLINE]

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