title: The prenylated dioxopiperazine alkaloid Cristatin A has selective telomeric DNA G-quadruplex stabilising properties.
abstract: Cristatin A (1a/b), a prenylated dioxopiperazine alkaloid, has been shown to bind selectively to telomeric quadruplex DNA using a FRET-based DNA melting assay. Crucially, the molecule is more drug-like than most previously identified quadruplex-binding agents, and provides a unique chemical scaffold for future chemical biology and drug discovery studies.
authors: Department of Pharmacy, King's College London, Stamford Street, London, SE18WA, UK.
authors: Khondaker M
authors: KM
authors: Rahman
authors: Mohammad D
authors: MD
authors: Hossain
authors: Mohammad H
authors: MH
authors: Sohrab
authors: Alex F
authors: AF
authors: Drake
authors: Tam T
authors: TT
authors: Bui
authors: Jarmila
authors: J
authors: Husby
authors: Mekala
authors: M
authors: Gunaratnam
authors: Stephen
authors: S
authors: Neidle
authors: Choudhury M
authors: CM
authors: Hasan
authors: David E
authors: DE
authors: Thurston
mesh_terms: D000045:Acacia / Q000737:chemistry*; D000470:Alkaloids / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D001665:Binding Sites; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000737:chemistry; D055808:Drug Discovery; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D009691:Nucleic Acid Denaturation; D018515:Plant Leaves / Q000737:chemistry; D016615:Telomere / Q000737:chemistry*; D014364:Tryptophan / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; C447012:cristatin A; D014364:Tryptophan; D004247:DNA; C427203:calf thymus DNA