[HTML][HTML] Chemical and structural studies provide a mechanistic basis for recognition of the MYC G-quadruplex

DR Calabrese, X Chen, EC Leon, SM Gaikwad… - Nature …, 2018 - nature.com
Abstract G-quadruplexes (G4s) are noncanonical DNA structures that frequently occur in the
promoter regions of oncogenes, such as MYC, and regulate gene expression. Although G4s …

Human MYC G-quadruplex: From discovery to a cancer therapeutic target

W Wang, S Hu, Y Gu, Y Yan, DB Stovall, D Li… - Biochimica et Biophysica …, 2020 - Elsevier
Overexpression of the MYC oncogene is a molecular hallmark of both cancer initiation and
progression. Targeting MYC is a logical and effective cancer therapeutic strategy. A special …

[HTML][HTML] G-Quadruplex: a regulator of gene expression and its chemical targeting

T Tian, YQ Chen, SR Wang, X Zhou - Chem, 2018 - cell.com
Summary G-quadruplex (G4) is an important type of nucleic acid secondary structure. An
abundance of potential G4-forming sites have been shown to exist in genomes, leading to …

Solution structure of a 2: 1 quindoline–c-MYC G-quadruplex: insights into G-quadruplex-interactive small molecule drug design

J Dai, M Carver, LH Hurley, D Yang - Journal of the American …, 2011 - ACS Publications
Unimolecular parallel-stranded G-quadruplex structures are found to be prevalent in gene
promoters. The nuclease hypersensitivity element III1 (NHE III1) of the c-MYC promoter can …

Structural recognition of the MYC promoter G-quadruplex by a quinoline derivative: insights into molecular targeting of parallel G-quadruplexes

J Dickerhoff, J Dai, D Yang - Nucleic Acids Research, 2021 - academic.oup.com
Abstract DNA G-Quadruplexes (G4s) formed in oncogene promoters regulate transcription.
The oncogene MYC promoter G4 (MycG4) is the most prevalent G4 in human cancers …

Cell penetrating thiazole peptides inhibit c-MYC expression via site-specific targeting of c-MYC G-quadruplex

D Dutta, M Debnath, D Müller, R Paul… - Nucleic acids …, 2018 - academic.oup.com
The structural differences among different G-quadruplexes provide an opportunity for site-
specific targeting of a particular G-quadruplex structure. However, majority of G-quadruplex …

G-quadruplex interacting small molecules and drugs: from bench toward bedside

S Müller, R Rodriguez - Expert review of clinical pharmacology, 2014 - Taylor & Francis
G-quadruplexes are non-Watson-Crick four-stranded nucleic acid structures. Recent
evidence points toward their existence in vivo and their implication in various biological …

Recent Update on Targeting c-MYC G-Quadruplexes by Small Molecules for Anticancer Therapeutics

R Chaudhuri, S Bhattacharya, J Dash… - Journal of Medicinal …, 2020 - ACS Publications
Guanine-rich DNA sequences have the propensity to adopt four-stranded tetrahelical G-
quadruplex (G4) structures that are overrepresented in gene promoters. The structural …

Stabilization and structure of telomeric and c-myc region intramolecular G-quadruplexes: the role of central cations and small planar ligands

V Gabelica, E Shammel Baker… - Journal of the …, 2007 - ACS Publications
A promising approach for anticancer strategies is the stabilization of telomeric DNA into a G-
quadruplex structure. To explore the intrinsic stabilization of folded G-quadruplexes, we …

[HTML][HTML] A G-quadruplex-binding compound showing anti-tumour activity in an in vivo model for pancreatic cancer

SA Ohnmacht, C Marchetti, M Gunaratnam… - Scientific reports, 2015 - nature.com
We report here that a tetra-substituted naphthalene-diimide derivative (MM41) has
significant in vivo anti-tumour activity against the MIA PaCa-2 pancreatic cancer xenograft …