title: Identification of a naturally occurring quinazolin-4(3H)-one firefly luciferase inhibitor.
abstract: A prefractionated Streptomyces-derived extract was initially identified as being active using a luciferase-based AMP-activated protein kinase (AMPK) assay. Bioassay-guided fractionation led to the isolation of the new compound quinazolin-4(3H)-one (1) as the active component. However, 1 was shown to have potent firefly luciferase inhibitory activity with no effect on AMPK. This is the first report of a natural luciferase inhibitor.
authors.affiliation: MerLion Pharmaceuticals, 1 Science Park Road, The Capricorn #05-01, Singapore Science Park II 117528, Singapore. brinda@merlionpharma.com
authors.forename: Brinda
authors.initials: B
authors.lastname: Somanadhan
authors.forename: Chungyan
authors.initials: C
authors.lastname: Leong
authors.forename: Stephen R
authors.initials: SR
authors.lastname: Whitton
authors.forename: Siewbee
authors.initials: S
authors.lastname: Ng
authors.forename: Antony D
authors.initials: AD
authors.lastname: Buss
authors.forename: Mark S
authors.initials: MS
authors.lastname: Butler
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000378:metabolism*; D000818:Animals; D001688:Biological Products / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D049409:Luciferases, Firefly / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D052999:Quinazolinones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D013302:Streptomyces / Q000737:chemistry*
chemical_list: C561170:2-(4'-(methylamino)phenyl)quinazolin-4(3H)-one; D001688:Biological Products; D052999:Quinazolinones; D049409:Luciferases, Firefly; D055372:AMP-Activated Protein Kinases