Research output: Contribution to journal › Article › peer-review
Discovery of Strecker-type alpha-aminonitriles as a new class of human carbonic anhydrase inhibitors using differential scanning fluorimetry. / Krasavin, Mikhail; Stavniichuk, Roman; Zozulya, Sergey; Borysko, Petro; Vullo, Daniela; Supuran, Claudiu T.
In: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 31, No. 6, 2016, p. 1707-1711.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Discovery of Strecker-type alpha-aminonitriles as a new class of human carbonic anhydrase inhibitors using differential scanning fluorimetry
AU - Krasavin, Mikhail
AU - Stavniichuk, Roman
AU - Zozulya, Sergey
AU - Borysko, Petro
AU - Vullo, Daniela
AU - Supuran, Claudiu T.
PY - 2016
Y1 - 2016
N2 - 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.
AB - 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.
KW - Carbonic anhydrases
KW - cyanide donors
KW - differential scanning fluorimetry
KW - isoform selectivity
KW - protein affinity
KW - suicide inhibitors
KW - thermal shift assay
KW - IX
KW - STABILITY
KW - AFFINITY
KW - DESIGN
KW - SITE
U2 - 10.3109/14756366.2016.1156676
DO - 10.3109/14756366.2016.1156676
M3 - статья
VL - 31
SP - 1707
EP - 1711
JO - Journal of Enzyme Inhibition and Medicinal Chemistry
JF - Journal of Enzyme Inhibition and Medicinal Chemistry
SN - 1475-6366
IS - 6
ER -
ID: 9433063