title: Discovery of Strecker-type α-aminonitriles as a new class of human carbonic anhydrase inhibitors using differential scanning fluorimetry.
abstract: A new type of carbonic anhydrase inhibitors was identified via differential scanning fluorimetry (DSF) screening. The compounds displayed interesting inhibition profile against human carbonic anhydrase isoforms I, II, IX and XII with an obvious selectivity displayed by one compound toward carbonic anhydrase (CA) IX, an established anti-cancer target. A hypothetical mechanism of inhibitory action by the Strecker-type α-aminonitriles has been proposed.
authors.affiliation: a Institute of Chemistry and Translational Biomedicine, Saint Petersburg State University , Peterhof , Russian Federation .
authors.forename: Mikhail
authors.initials: M
authors.lastname: Krasavin
authors.affiliation: b Enamine Ltd , Kyiv , Ukraine .
authors.forename: Roman
authors.initials: R
authors.lastname: Stavniichuk
authors.affiliation: b Enamine Ltd , Kyiv , Ukraine .|c Taras Shevchenko National University , Kyiv , Ukraine , and.
authors.forename: Sergey
authors.initials: S
authors.lastname: Zozulya
authors.affiliation: b Enamine Ltd , Kyiv , Ukraine .
authors.forename: Petro
authors.initials: P
authors.lastname: Borysko
authors.affiliation: d Neurofarba Department, Universita degli Studi di Firenze , Florence , Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Vullo
authors.affiliation: d Neurofarba Department, Universita degli Studi di Firenze , Florence , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D005470:Fluorometry / Q000379:methods*; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D009570:Nitriles
keywords: Carbonic anhydrases; cyanide donors; differential scanning fluorimetry; isoform selectivity; protein affinity; suicide inhibitors; thermal shift assay