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

Autor:	Jyotirmayee Dash, Santanu Bhattacharya, Ritapa Chaudhuri, Semantee Bhattacharya
Rok vydání:	2020
Předmět:	Nuclease biology Oncogene Chemistry Promoter Computational biology G-quadruplex Small molecule Drug development Drug Discovery Gene expression biology.protein Molecular Medicine Gene
Zdroj:	Journal of Medicinal Chemistry. 64:42-70
ISSN:	1520-4804 0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::703e701454235f1971b973525955f896 https://doi.org/10.1021/acs.jmedchem.0c01145 Zobrazit plný text záznamu