title: Firefly luciferase inhibition.
abstract: Firefly luciferase (Luc) is the most studied of the luciferase enzymes and the mechanism and kinetics of the reactions catalyzed by this enzyme have been relatively well characterized. Luc catalyzes the bioluminescent reaction involving firefly luciferin (D-LH(2)), adenosine triphosphate (ATP), magnesium ion and molecular oxygen with the formation of an electronically excited species (oxyluciferin), inorganic pyrophosphate (PPi), carbon dioxide and adenosine monophosphate (AMP). Luc also catalyzes other non-luminescent reactions, which can interfere with the light production mechanism. Following electronic relaxation, the excited oxyluciferin emits radiation in the visible region of the electromagnetic spectrum (550-570 nm). Among the various possible compounds, several classes of inhibitory substances interfere with the activity of this enzyme: here, we consider substrate-related compounds, intermediates or products of the Luc catalyzed reactions, in addition to anesthetics and, fatty acids. This review summarizes the main inhibitors of Luc and the corresponding inhibition kinetic parameters.
authors.affiliation: Centro de Investigação em Química (CIQ-UP), Grupo de Ciências Biológicas e Bioanalíticas, Faculdade de Farmácia da Universidade de Coimbra, Polo das Ciências da Saúde, 3000-548 Coimbra, Portugal.
authors.forename: João M M
authors.initials: JM
authors.lastname: Leitão
authors.forename: Joaquim C G
authors.initials: JC
authors.lastname: Esteves da Silva
mesh_terms: D000473:Alkanes / Q000737:chemistry; D000777:Anesthetics / Q000737:chemistry; D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry; D002384:Catalysis; D004791:Enzyme Inhibitors / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry; D048888:Fireflies / Q000201:enzymology; D007211:Indoles / Q000737:chemistry / Q000378:metabolism; D049409:Luciferases, Firefly / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011719:Pyrazines / Q000737:chemistry / Q000378:metabolism
chemical_list: D000473:Alkanes; D000777:Anesthetics; D052160:Benzothiazoles; D004791:Enzyme Inhibitors; D005227:Fatty Acids; D007211:Indoles; D011719:Pyrazines; C014730:oxyluciferin; D049409:Luciferases, Firefly; C005465:benzothiazole