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

Chaudhuri, Ritapa ; Bhattacharya, Semantee ; Dash, Jyotirmayee ; Bhattacharya, Santanu (2021) Recent Update on Targeting c-MYC G-Quadruplexes by Small Molecules for Anticancer Therapeutics Journal of Medicinal Chemistry, 64 (1). pp. 42-70. ISSN 0022-2623

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Official URL: http://doi.org/10.1021/acs.jmedchem.0c01145

Related URL: http://dx.doi.org/10.1021/acs.jmedchem.0c01145

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 thec-MYC 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.

Item Type:Article
Source:Copyright of this article belongs to American Chemical Society.
ID Code:134276
Deposited On:06 Jan 2023 03:41
Last Modified:06 Jan 2023 03:41

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