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

Research output: Contribution to journal › Article › peer-review

Laboratory of Chemical Pharmacology

DOI

https://doi.org/10.3109/14756366.2016.1156676
Final published version
https://doi.org/10.3109/14756366.2016.1156676
Final published version

Mikhail Krasavin
Roman Stavniichuk
Sergey Zozulya
Petro Borysko
Daniela Vullo
Claudiu T. Supuran

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 alpha-aminonitriles has been proposed.

Original language	English
Pages (from-to)	1707-1711
Number of pages	5
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume	31
Issue number	6
DOIs	https://doi.org/10.3109/14756366.2016.1156676 https://doi.org/10.3109/14756366.2016.1156676
State	Published - 2016

Research areas

Carbonic anhydrases, cyanide donors, differential scanning fluorimetry, isoform selectivity, protein affinity, suicide inhibitors, thermal shift assay, IX, STABILITY, AFFINITY, DESIGN, SITE

ID: 9433063