Literature DB >> 26983069

Discovery of Strecker-type α-aminonitriles as a new class of human carbonic anhydrase inhibitors using differential scanning fluorimetry.

Mikhail Krasavin1, Roman Stavniichuk2, Sergey Zozulya2,3, Petro Borysko2, Daniela Vullo4, Claudiu T Supuran4.   

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.

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Keywords:  Carbonic anhydrases; cyanide donors; differential scanning fluorimetry; isoform selectivity; protein affinity; suicide inhibitors; thermal shift assay

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Year:  2016        PMID： 26983069     DOI： 10.3109/14756366.2016.1156676

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN： 1475-6366            Impact factor:   5.051


  2 in total

1.  Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement.

Authors:  Mikhail Krasavin; Stanislav Kalinin; Sergey Zozulya; Anastasia Griniukova; Petro Borysko; Andrea Angeli; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

2.  Screening of benzenesulfonamide in combination with chemically diverse fragments against carbonic anhydrase by differential scanning fluorimetry.

Authors:  Mikhail Krasavin; Stanislav Kalinin; Sergey Zozulya; Anastasiia Gryniukova; Petro Borysko; Andrea Angeli; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
  2 in total

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