Indenoisoquinoline Topoisomerase Inhibitors Strongly Bind and Stabilize the MYC Promoter G-Quadruplex and Downregulate MYC

KB Wang, MSA Elsayed, G Wu, N Deng… - Journal of the …, 2019 - ACS Publications
MYC is one of the most important oncogenes and is overexpressed in the majority of
cancers. G-Quadruplexes are noncanonical four-stranded DNA secondary structures that …

DNA G-quadruplex in human telomeres and oncogene promoters: structures, functions, and small molecule targeting

L Chen, J Dickerhoff, S Sakai… - Accounts of chemical …, 2022 - ACS Publications
Conspectus DNA G-quadruplex secondary structures formed in guanine-rich human
telomeres and oncogene promoters are functionally important and have emerged as a …

Targeting Promoter G‐Quadruplex DNAs by Indenopyrimidine‐Based Ligands

KV Diveshkumar, S Sakrikar, S Harikrishna… - …, 2014 - Wiley Online Library
The formation of G‐quadruplex structures can regulate telomerase activity and the
expression of oncogenes at the transcriptional and translational levels. Therefore …

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 …

Design, Synthesis, and Evaluation of Isaindigotone Derivatives To Downregulate c-myc Transcription via Disrupting the Interaction of NM23-H2 with G-Quadruplex

C Shan, JW Yan, YQ Wang, T Che… - Journal of Medicinal …, 2017 - ACS Publications
Transcriptional control of c-myc oncogene is an important strategy for antitumor drug design.
G-quadruplexes in the promoter region have been proven to be the transcriptional down …

Anticancer activity and cellular repression of c-MYC by the G-quadruplex-stabilizing 11-piperazinylquindoline is not dependent on direct targeting of the G-quadruplex …

PVL Boddupally, S Hahn, C Beman, B De… - Journal of medicinal …, 2012 - ACS Publications
This G-rich region of the c-MYC promoter has been shown to form a G-quadruplex structure
that acts as a silencer element for c-MYC transcriptional control. In the present work, we …

Design and synthesis of indenoisoquinolines targeting topoisomerase I and other biological macromolecules for cancer chemotherapy

M Cushman - Journal of Medicinal Chemistry, 2021 - ACS Publications
The discovery that certain indenoisoquinolines inhibit the religation reaction of DNA in the
topoisomerase I-DNA-indenoisoquinoline ternary complex led to a structure-based drug …

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 …

Targeting the c-Kit Promoter G-quadruplexes with 6-Substituted Indenoisoquinolines

M Bejugam, M Gunaratnam, S Müller… - ACS medicinal …, 2010 - ACS Publications
Herein, we demonstrate the design, synthesis, biophysical properties, and preliminary
biological evaluation of 6-substituted indenoisoquinolines as a new class of G-quadruplex …

Inhibition of myc promoter and telomerase activity and induction of delayed apoptosis by SYUIQ-5, a novel G-quadruplex interactive agent in leukemia cells

JN Liu, R Deng, JF Guo, JM Zhou, GK Feng, ZS Huang… - Leukemia, 2007 - nature.com
ABL. 2, 3 C-myc is an important proto-oncogene, which is linked to potentiation of cellular
proliferation and to inhibition of differentiation and acts as both a transcriptional activator and …