Ontology highlight
ABSTRACT:
SUBMITTER: Calabrese DR
PROVIDER: S-EPMC6185959 | biostudies-literature | 2018 Oct
REPOSITORIES: biostudies-literature
Calabrese David R DR Chen Xiang X Leon Elena C EC Gaikwad Snehal M SM Phyo Zaw Z Hewitt William M WM Alden Stephanie S Hilimire Thomas A TA He Fahu F Michalowski Aleksandra M AM Simmons John K JK Saunders Lindsey B LB Zhang Shuling S Connors Daniel D Walters Kylie J KJ Mock Beverly A BA Schneekloth John S JS
Nature communications 20181012 1
G-quadruplexes (G4s) are noncanonical DNA structures that frequently occur in the promoter regions of oncogenes, such as MYC, and regulate gene expression. Although G4s are attractive therapeutic targets, ligands capable of discriminating between different G4 structures are rare. Here, we describe DC-34, a small molecule that potently downregulates MYC transcription in cancer cells by a G4-dependent mechanism. Inhibition by DC-34 is significantly greater for MYC than other G4-driven genes. We us ...[more]