Molecular cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
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Hewitson KS, Vullo D, Scozzafava A, Mastrolorenzo A, Supuran CT
Molecular cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Malassezia globosa, a potential antidandruff target.
J Med Chem. 2012 Apr 12;55(7):3513-20. doi: 10.1021/jm300203r. Epub 2012 Mar 28.
- PubMed ID
- 22424239 [ View in PubMed]
- Abstract
A beta-carbonic anhydrase (CA, EC 4.2.1.1) from the fungal pathogen Malassezia globosa has been cloned, characterized, and studied for its inhibition with sulfonamides. This enzyme, designated MG-CA, has significant catalytic activity in the CO(2) hydration reaction and was inhibited by sulfonamides, sulfamates, and sulfamides with K(I) in the nanomolar to micromolar range. Several sulfonamides have also been investigated for the inhibition of growth of M. globosa, M. dermatis, M. pachydermatic, and M. furfur in cultures, whereas a mouse model of dandruff showed that treatment with sulfonamides led to fragmented fungal hyphae, as for the treatment with ketoconazole, a clinically used antifungal agent. These data prompt us to propose MG-CA as a new antidandruff drug target.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 3-[4-(AMINOSULFONYL)PHENYL]PROPANOIC ACID Carbonic anhydrase 2 Ki (nM) 495 N/A N/A Details 4-(2-AMINOETHYL)BENZENESULFONAMIDE Carbonic anhydrase 2 Ki (nM) 160 N/A N/A Details 5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide Carbonic anhydrase 2 Ki (nM) 12 N/A N/A Details 5-[(phenylsulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamide Carbonic anhydrase 2 Ki (nM) 9 N/A N/A Details Acetazolamide Carbonic anhydrase 1 Ki (nM) 250 N/A N/A Details Acetazolamide Carbonic anhydrase 2 Ki (nM) 12 N/A N/A Details Brinzolamide Carbonic anhydrase 2 Ki (nM) 3 N/A N/A Details Celecoxib Carbonic anhydrase 2 Ki (nM) 21 N/A N/A Details Diclofenamide Carbonic anhydrase 2 Ki (nM) 38 N/A N/A Details Dorzolamide Carbonic anhydrase 2 Ki (nM) 9 N/A N/A Details Ethoxzolamide Carbonic anhydrase 2 Ki (nM) 8 N/A N/A Details Sulpiride Carbonic anhydrase 2 Ki (nM) 40 N/A N/A Details Topiramate Carbonic anhydrase 2 Ki (nM) 10 N/A N/A Details Valdecoxib Carbonic anhydrase 2 Ki (nM) 43 N/A N/A Details Zonisamide Carbonic anhydrase 2 Ki (nM) 35 N/A N/A Details