title: A Fluorescent Anti-Cancer Agent, 3,6-bis(1-methyl-4-vinylpyridinium) Carbazole Diiodide, Stains G-Quadruplexes in Cells and Inhibits Tumor Growth.
abstract: Compelling evidence suggests that formation of guanine-quadruplex (G4) can protect the integrity of chromosome ends in eukaryotes, and regulate the activity of some gene promoters. In addition, G4 may be a novel therapeutic target. Thus, a number of ligands have been synthesized to stabilize G4. However, skepticism lingers over the existence of G4 in cells, as well as its biological function. The molecule 3,6-bis(1-methyl-4-vinylpyridium) carbazole diiodide (BMVC) can be used not only as a fluorescent probe to map endogenous and exogenous G4 in live cells, but also as therapeutic agent that arrests cancer growth by inhibiting telomerase activity and regulating gene expression. Thus, the fluorescence of a G4 anti-cancer agent is an invaluable tool to detect G4 in cells, investigate ligand-G4 interaction in live cells, examine the biological function of G4, and guide the development of new fluorescent anti-cancer agents.
authors.forename: Ting-Yuan
authors.initials: TY
authors.lastname: Tse
authors.forename: Cheng-Chung
authors.initials: CC
authors.lastname: Chang
authors.forename: Jing-Jer
authors.initials: JJ
authors.lastname: Lin
authors.affiliation: Institute of Atomic and Molecular Sciences, Academia Sinica, Taipei 10617, Taiwan, P.R. China. tcchang@po.iams.sinica.edu.tw.
authors.forename: Ta-Chau
authors.initials: TC
authors.lastname: Chang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000032:analysis* / Q000737:chemistry / Q000494:pharmacology*; D002227:Carbazoles / Q000032:analysis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D005453:Fluorescence; D054856:G-Quadruplexes; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics* / Q000473:pathology; D011726:Pyridinium Compounds / Q000032:analysis* / Q000737:chemistry / Q000494:pharmacology*; D013194:Staining and Labeling; D013329:Structure-Activity Relationship
chemical_list: C486012:3,6-bis(1-methyl-4-vinylpyridium)carbazole diiodide; D000970:Antineoplastic Agents; D002227:Carbazoles; D011726:Pyridinium Compounds