| Literature DB >> 26174556 |
Daniela Vullo1, Viviana De Luca2, Sonia Del Prete3, Vincenzo Carginale2, Andrea Scozzafava1, Clemente Capasso4, Claudiu T Supuran5.
Abstract
The Antarctic bacterium Pseudoalteromonas haloplanktis encodes for a γ-class carbonic anhydrase (CA, EC 4.2.1.1), which was cloned, purified and characterized. The enzyme (PhaCAγ) has a good catalytic activity for the physiologic reaction of CO2 hydration to bicarbonate and protons, with a k(cat) of 1.4×10(5) s(-1) and a k(cat)/K(m) of 1.9×10(6) M(-1)×s(-1). A series of sulfonamides and a sulfamate were investigated as inhibitors of the new enzyme. Methazolamide and indisulam showed the best inhibitory properties (K(I)s of 86.7-94.7 nM). This contribution shed new light on γ-CAs inhibition profiles with a relevant class of pharmacologic agents.Entities:
Keywords: Antarctic carbonic anhydrase; Carbonic anhydrase; Cold adaptation; Cold enzymes; Hydratase activity; Inhibitors; Metalloenzymes; Psychrophiles; Sulfonamide
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Year: 2015 PMID： 26174556 DOI： 10.1016/j.bmcl.2015.06.079
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823