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.
Carbonic anhydrase inhibitors and activators for novel therapeutic applications / C. T. Supuran. - In: FUTURE MEDICINAL CHEMISTRY. - ISSN 1756-8919. - STAMPA. - 3:(2011), pp. 1165-1180. [10.4155/fmc.11.69]
Carbonic anhydrase inhibitors and activators for novel therapeutic applications.
SUPURAN, CLAUDIU TRANDAFIR
2011
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.I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.