Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.

Article Details

Citation

Bertucci A, Innocenti A, Scozzafava A, Tambutte S, Zoccola D, Supuran CT

Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):710-4. doi: 10.1016/j.bmcl.2010.11.124. Epub 2010 Dec 4.

PubMed ID
21208801 [ View in PubMed
]
Abstract

The catalytic activity and the inhibition of a new coral carbonic anhydrase (CA, EC 4.2.1.1), from the scleractinian coral Stylophora pistillata, STPCA-2, has been investigated. STPCA-2 has high catalytic activity for the physiological reaction being less sensitive to anion and sulfonamide inhibitors compared to STPCA, a coral enzyme previously described. The best STPCA-2 anion inhibitors were sulfamide, sulfamic acid, phenylboronic acid, and phenylarsonic acid (K(I)s of 5.7-67.2muM) whereas the best sulfonamide inhibitors were acetazolamide and dichlorophenamide (K(I)s of 74-79nM). Because this discriminatory effect between these two coral CAs, sulfonamides may be useful to better understand the physiological role of STPCA and STPCA-2 in corals and biomineralization processes.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
3-[4-(AMINOSULFONYL)PHENYL]PROPANOIC ACIDCarbonic anhydrase 1Ki (nM)6690N/AN/ADetails
3-[4-(AMINOSULFONYL)PHENYL]PROPANOIC ACIDCarbonic anhydrase 2Ki (nM)495N/AN/ADetails
4-(2-AMINOETHYL)BENZENESULFONAMIDECarbonic anhydrase 2Ki (nM)160N/AN/ADetails
5-[(phenylsulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamideCarbonic anhydrase 2Ki (nM)9N/AN/ADetails
AcetazolamideCarbonic anhydrase 1Ki (nM)250N/AN/ADetails
AcetazolamideCarbonic anhydrase 2Ki (nM)12N/AN/ADetails
BrinzolamideCarbonic anhydrase 1Ki (nM)45000N/AN/ADetails
BrinzolamideCarbonic anhydrase 2Ki (nM)3N/AN/ADetails
CelecoxibCarbonic anhydrase 2Ki (nM)21N/AN/ADetails
DiclofenamideCarbonic anhydrase 1Ki (nM)1200N/AN/ADetails
DiclofenamideCarbonic anhydrase 2Ki (nM)38N/AN/ADetails
DorzolamideCarbonic anhydrase 1Ki (nM)50000N/AN/ADetails
DorzolamideCarbonic anhydrase 2Ki (nM)9N/AN/ADetails
EthoxzolamideCarbonic anhydrase 1Ki (nM)25N/AN/ADetails
EthoxzolamideCarbonic anhydrase 2Ki (nM)8N/AN/ADetails
SulpirideCarbonic anhydrase 2Ki (nM)40N/AN/ADetails
SulthiameCarbonic anhydrase 2Ki (nM)9N/AN/ADetails
TopiramateCarbonic anhydrase 1Ki (nM)250N/AN/ADetails
TopiramateCarbonic anhydrase 2Ki (nM)10N/AN/ADetails
ValdecoxibCarbonic anhydrase 2Ki (nM)43N/AN/ADetails
ZonisamideCarbonic anhydrase 1Ki (nM)56N/AN/ADetails
ZonisamideCarbonic anhydrase 2Ki (nM)35N/AN/ADetails