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, CO2 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.