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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 principle that c-MYC transcription can be controlled by ligand-mediated G-quadruplex stabilization is established, establishing the principle that the purine-rich strand of the DNA in this region can form two different intramolecular G- quadruplex structures.
DNA and its associated processes as targets for cancer therapy
  • L. Hurley
  • Biology, Medicine
    Nature Reviews Cancer
  • 1 March 2002
A new generation of agents that target DNA-associated processes are anticipated to be far more specific and effective in cancer therapeutics.
Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
The evidence for G-quadruplexes in gene promoters is described and their potential as therapeutic targets are discussed, as well as progress in the development of strategies to harness this potential through intervention with small-molecule ligands.
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
Significantly, a striking hypersensitivity to both nucleases was observed at the 3′-side residue of the predicted G-quadruplex-forming region in the presence of KCl and telomestatin, indicating altered conformation of the human VEGF proximal promoter region surrounding the guanine-rich sequence.
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), and it is believed that TMPyP4 in decreasing both c-MYC protein levels and telomerase activity, as well as its anticancer effects in vivo, is a worthwhile agent to pursue and develop further.
G-quadruplex DNA: a potential target for anti-cancer drug design.
  • H. Han, L. Hurley
  • Medicine, Biology
    Trends in pharmacological sciences
  • 1 April 2000
The possible role of G-quadruplex-interactive compounds as pharmacologically important molecules is explored in this article.
Structures, folding patterns, and functions of intramolecular DNA G-quadruplexes found in eukaryotic promoter regions.
Recent studies on intramolecular G-quadruplex structures that form in the promoter regions of some human genes in living cells are examined and the biological implications of these structures are discussed.
Identification and Characterization of Nucleolin as a c-myc G-quadruplex-binding Protein*
myc is a proto-oncogene that plays an important role in the promotion of cellular growth and proliferation. Understanding the regulation of c-myc is important in cancer biology, as it is
The role of supercoiling in transcriptional control of MYC and its importance in molecular therapeutics
This work has demonstrated that supercoiling that is induced by transcription has been demonstrated to have dynamic effects on DNA in the MYC promoter element: it converts duplex DNA to non-duplex DNA structures, even at considerable distances from the transcriptional start site.
Deconvoluting the structural and drug-recognition complexity of the G-quadruplex-forming region upstream of the bcl-2 P1 promoter.
It is demonstrated that the guanine-rich strand of the DNA in this region can form any one of three distinct intramolecular G- quadruplex structures, and the complexity of the G-quadruplexes in the bcl-2 promoter extends to each having the capacity to form either three or six different loop isomers.