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Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription
The nuclease hypersensitivity element III1 upstream of the P1 promoter of c-MYC controls 85–90% of the transcriptional activation of this gene. We have demonstrated that the purine-rich strand of theExpand
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DNA and its associated processes as targets for cancer therapy
  • L. Hurley
  • Biology, Medicine
  • Nature Reviews Cancer
  • 1 March 2002
DNA is the molecular target for many of the drugs that are used in cancer therapeutics, and is viewed as a non-specific target of cytotoxic agents. Although this is true for traditionalExpand
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Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
G-quadruplexes are four-stranded DNA structures that are over-represented in gene promoter regions and are viewed as emerging therapeutic targets in oncology, as transcriptional repression ofExpand
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Facilitation of a structural transition in the polypurine/polypyrimidine tract within the proximal promoter region of the human VEGF gene by the presence of potassium and G-quadruplex-interactive
The proximal promoter region of the human vascular endothelial growth factor (VEGF) gene contains a polypurine/polypyrimidine tract that serves as a multiple binding site for Sp1 and Egr-1Expand
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The cationic porphyrin TMPyP4 down-regulates c-MYC and human telomerase reverse transcriptase expression and inhibits tumor growth in vivo.
Cationic porphyrins are being studied as possible anticancer agents because of their ability to bind to and stabilize DNA guanine quadruplexes (G-quadruplexes). We have shown previously that theExpand
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The importance of negative superhelicity in inducing the formation of G-quadruplex and i-motif structures in the c-Myc promoter: implications for drug targeting and control of gene expression.
  • D. Sun, L. Hurley
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 14 May 2009
The importance of DNA supercoiling in transcriptional regulation has been known for many years, and more recently, transcription itself has been shown to be a source of this superhelicity. To mimicExpand
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The role of supercoiling in transcriptional control of MYC and its importance in molecular therapeutics
MYC is deregulated in most tumour types, but an effective means to selectively target its aberrant expression is not yet available. Supercoiling that is induced by transcription has been demonstratedExpand
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Structures, folding patterns, and functions of intramolecular DNA G-quadruplexes found in eukaryotic promoter regions.
In its simplest form, a DNA G-quadruplex is a four-stranded DNA structure that is composed of stacked guanine tetrads. G-quadruplex-forming sequences have been identified in eukaryotic telomeres, asExpand
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NMR solution structure of the major G-quadruplex structure formed in the human BCL2 promoter region
BCL2 protein functions as an inhibitor of cell apoptosis and has been found to be aberrantly expressed in a wide range of human diseases. A highly GC-rich region upstream of the P1 promoter plays anExpand
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G-quadruplex DNA: a potential target for anti-cancer drug design.
  • H. Han, L. Hurley
  • Medicine, Biology
  • Trends in pharmacological sciences
  • 1 April 2000
In addition to the familiar duplex DNA, certain DNA sequences can fold into secondary structures that are four-stranded; because they are made up of guanine (G) bases, such structures are calledExpand
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