caa a22 4500 445878916 CHVBK 20180317145536.0 cr unu---uuuuu 170323e20110501xx s 000 0 eng 10.1007/s11030-010-9271-4 doi (NATIONALLICENCE)springer-10.1007/s11030-010-9271-4 Supuran Claudiu Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Rm. 188, Via della Lastruccia 3, 50019, Sesto Fiorentino (Firenze), Italy aut Carbonic anhydrase inhibition with natural products: novel chemotypes and inhibition mechanisms [Elektronische Daten] [Claudiu Supuran] Five genetically distinct classes of carbonic anhydrases (CAs, EC 4.2.1.1) are present in organisms all over the phylogenetic tree (α-, β-, γ-, δ-, and ζ-families). These metalloenzymes catalyze CO2 hydration to bicarbonate and protons. Inhibition of α-CAs from vertebrates, including humans, with sulfonamides was exploited clinically for decades for various classes of diuretics and systemically acting antiglaucoma agents, whereas newer inhibitors are used as topically acting antiglaucoma drugs, anticonvulsants, antiobesity, antipain and antitumor agents/diagnostic tools. Recently, novel interesting chemotypes, in addition to the sulfonamide and sulfamate were discovered, many of which are based on natural products, such as phenols/polyphenols, phenolic acids, and coumarins. Their detailed mechanism of inhibition has been explained by means of kinetic and X-ray crystallographic studies, and can be used for the rational drug design of other agents. Possible applications for these new chemotypes in drug design of CA inhibitors are envisaged and discussed in detail in this review. Springer Science+Business Media B.V., 2010 Carbonic anhydrase nationallicence Zinc enzyme nationallicence Enzyme inhibitor nationallicence Phenols nationallicence Polyphenols nationallicence Natural product nationallicence Coumarin nationallicence Polyamine nationallicence Spermine nationallicence Spermidine nationallicence Molecular Diversity Springer Netherlands 15/2(2011-05-01), 305-316 1381-1991 15:2<305 2011 15 11030 https://doi.org/10.1007/s11030-010-9271-4 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11030-010-9271-4 text/html Onlinezugriff via DOI NATIONALLICENCE 100 1- Supuran Claudiu Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Rm. 188, Via della Lastruccia 3, 50019, Sesto Fiorentino (Firenze), Italy aut NATIONALLICENCE 773 0- Molecular Diversity Springer Netherlands 15/2(2011-05-01), 305-316 1381-1991 15:2<305 2011 15 11030 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer