title: Carbonic anhydrase inhibitors and activators for novel therapeutic applications.
abstract: Carbonic anhydrases (CAs, Enzyme Commission number 4.2.1.1) catalyze a simple but fundamental reaction, CO(2) hydration to yield bicarbonate and protons. CAs belonging to the α-, β-, γ-, δ- and ζ-families are found in many organisms all over the phylogenetic tree and their inhibition/activation have been studied in detail, leading to various therapeutic applications. Inhibition of mammalian α-CAs is exploited by some diuretics, whereas antiglaucoma, anticonvulsant, anti-obesity, altitude sickness and anti-tumor drugs/diagnostic agents target various of the 15 isoforms described so far in these organisms. Activation of some CAs may also have applications in therapy. Bacterial and fungal β-CA inhibitors or nematode α-CA inhibitors have been described that may lead to novel classes of anti-infectives.
authors.affiliation: Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino, Firenze, Italy. claudiu.supuran@unifi.it
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002256:Carbonic Anhydrases / Q000737:chemistry / Q000378:metabolism*; D002384:Catalysis; D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects*; D006801:Humans; D058990:Molecular Targeted Therapy; D020033:Protein Isoforms; D013096:Spermine / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D020033:Protein Isoforms; D013096:Spermine; D002256:Carbonic Anhydrases