title: Herbicide oryzalin inhibits human carbonic anhydrases in vitro.
abstract: Herbicides of the dinitroaniline chemical class, widely used oryzalin and trifluralin, and also nitralin were tested as inhibitors of recombinant human carbonic anhydrases (CAs). Oryzalin bound and inhibited 11 out of 12 catalytically active CA isoforms present in the human body with the affinities in the same range as clinically used CA drugs, while no effect was detected for the other two compounds. Binding of all three herbicides was examined by fluorescence-based thermal shift assay, isothermal titration calorimetry, and the inhibition of carbon dioxide hydratase activity. During the last decade, dinitroaniline compound-based therapies against protozoan diseases are being developed. Therefore, it is important to investigate their potential off-target effects, including human CAs.
authors.affiliation: Department of Biothermodynamics and Drug Design, Institute of Biotechnology, Vilnius University, Vilnius, LT-10257, Lithuania.
authors.forename: Lina
authors.initials: L
authors.lastname: Baranauskiene
authors.affiliation: Department of Biothermodynamics and Drug Design, Institute of Biotechnology, Vilnius University, Vilnius, LT-10257, Lithuania.
authors.forename: Daumantas
authors.initials: D
authors.lastname: Matulis
mesh_terms: D000086:Acetazolamide / Q000737:chemistry / Q000494:pharmacology; D000814:Aniline Compounds / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D002151:Calorimetry; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D004136:Dinitrobenzenes / Q000737:chemistry / Q000494:pharmacology*; D006540:Herbicides / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D007700:Kinetics; D015394:Molecular Structure; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D013424:Sulfanilamides / Q000737:chemistry / Q000494:pharmacology*; D017186:Titrimetry; D014274:Trifluralin / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000814:Aniline Compounds; D000981:Antiprotozoal Agents; D002257:Carbonic Anhydrase Inhibitors; D004136:Dinitrobenzenes; D006540:Herbicides; D007527:Isoenzymes; D011994:Recombinant Proteins; D013424:Sulfanilamides; C012465:oryzalin; C003499:nitralin; D014274:Trifluralin; D002256:Carbonic Anhydrases; D000086:Acetazolamide
keywords: carbonic anhydrase; herbicide; isothermal titration calorimetry; oryzalin; trifluralin