Targeting MYC expression through G-quadruplexes

TA Brooks, LH Hurley - Genes & cancer, 2010 - journals.sagepub.com
MYC expression that involves a four-stranded DNA structure, termed a G-quadruplex, amenable
to small molecule targeting. … the NHE III 1 in the MYC promoter are the closest thing that …

[HTML][HTML] Small molecules targeting c-Myc oncogene: promising anti-cancer therapeutics

BJ Chen, YL Wu, Y Tanaka, W Zhang - International journal of …, 2014 - ncbi.nlm.nih.gov
… and therapeutic strategies against cancer using small molecules targeting the oncogene, …
of agents targeting c-Myc, in particular G-quadruplexes formed in c-Myc promoter and c-Myc/…

[HTML][HTML] Mission possible: advances in MYC therapeutic targeting in cancer

BL Allen-Petersen, RC Sears - BioDrugs, 2019 - Springer
MYC:MAX complexes, reducing MYC promoter occupancy and effectively suppressing
transcription. A recent study from Jung et al. [59] demonstrated that under physiologic levels …

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
… important insights into targeting the major G4 of the MYC promoter by small molecules. The
newly … It has drug-like properties with low molecular weight, which makes it a promising lead-…

[HTML][HTML] MYC as a target for cancer treatment

MJ Duffy, S O'Grady, M Tang, J Crown - Cancer treatment reviews, 2021 - Elsevier
… of all 3 forms of MYC to their target promoters, has been shown to … targeting MYC has yet
progressed to clinical testing, APTO-253, which partly acts by decreasing expression of MYC, is …

[HTML][HTML] The action mechanism of the Myc inhibitor termed Omomyc may give clues on how to target Myc for cancer therapy

M Savino, D Annibali, N Carucci, E Favuzzi, MD Cole… - PloS one, 2011 - journals.plos.org
… To test whether the inhibition of nucleolin transactivation by Omomyc was due to a
reduction of promoter binding, we measured the amount of Myc bound to the nucleolin …

Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription

A Siddiqui-Jain, CL Grand… - Proceedings of the …, 2002 - National Acad Sciences
MYC expression is complex and involves multiple promoters and transcriptional start sites.
P1 and P2 seem to be the predominant promoters … -MYC promoter controls 85–90% of c-MYC

The role of supercoiling in transcriptional control of MYC and its importance in molecular therapeutics

TA Brooks, LH Hurley - Nature Reviews Cancer, 2009 - nature.com
… The particular transcriptional system we have described, the MYC promoter, is … -molecule
targeting, which provides several distinct advantages over oligomer targeting for molecular

Rational design of small-molecules to recognize G-quadruplexes of c-MYC promoter and telomere and the evaluation of their in vivo antitumor activity against breast …

W Long, BX Zheng, Y Li, XH Huang, DM Lin… - Nucleic acids …, 2022 - academic.oup.com
MYC overexpression (20). A few lately reported molecular binders that stabilize the c-MYC
promoter … 21–24), which supports that c-MYC could be an important drug target. The nuclease …

Gaining insights into the small molecule targeting of the G-quadruplex in the c-MYC promoter using NMR and an allele-specific transcriptional assay

CE Kaiser, V Gokhale, D Yang, LH Hurley - Quadruplex Nucleic Acids, 2013 - Springer
… characterization to target the G-quadruplex in the c-MYC promoter in an attempt to find
compounds that could down-regulate the expression of c-MYC at the transcriptional level. …