Recent update on targeting c-MYC G-quadruplexes by small molecules for anticancer therapeutics

Chaudhuri, R and Bhattacharya, S and Dash, J and Bhattacharya, S (2021) Recent update on targeting c-MYC G-quadruplexes by small molecules for anticancer therapeutics. In: Journal of Medicinal Chemistry, 64 (1). pp. 42-70.

PDF acs.jmedchem.0c01145.pdf - Published Version Restricted to Registered users only Download (4MB) | Request a copy

Abstract

Guanine-rich DNA sequences have the propensity to adopt four-stranded tetrahelical G-quadruplex (G4) structures that are overrepresented in gene promoters. The structural polymorphism and physicochemical properties of these non-Watson-Crick G4 structures make them important targets for drug development. The guanine-rich nuclease hypersensitivity element III1 present in the upstream of P1 promoter of c-MYC oncogene has the ability to form an intramolecular parallel G4 structure. The G4 structure that forms transiently in the c-MYC promoter functions as a transcriptional repressor element. The c-MYC oncogene is overexpressed in a wide variety of cancers and plays a key role in cancer progression. Till now, a large number of compounds that are capable of interacting and stabilizing thecMYC G4 have been reported. In this review, we summarize various c-MYC G4 specific molecules and discuss their effects on c-MYC gene expression in vitro and in vivo. © XXXX American Chemical Society.

Item Type:	Journal Article
Publication:	Journal of Medicinal Chemistry
Publisher:	American Chemical Society
Additional Information:	Copyright to this article belongs to American Chemical Society
Department/Centre:	Division of Chemical Sciences > Organic Chemistry
Date Deposited:	29 Jan 2021 05:23
Last Modified:	25 Jan 2023 12:25
URI:	https://eprints.iisc.ac.in/id/eprint/67821

Actions (login required)

View Item