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This chapter concerns influences of inhibitors and activators on carbonic anhydrase isoenzymes of various living systems. Carbonic anhydrase (EC 4.2.1.1., CA) is a pH regulatory/metabolic enzyme in all life kingdoms, found in organisms all over the phylogenetic tree (Supuran, 2008a,b,c) catalyzing the hydration of carbon dioxide to bicarbonate and the corresponding dehydration of bicarbonate in acidic medium with regeneration of CO2 (Sly and Hu, 1995). 16 isozymes have been described up to now in mammals, the most active ones as catalysts for carbon dioxide hydration being CA II and CA IX (Sly and Hu, 1995; Ozensoy et al., 2004; Bayram et al., 2008; Senturk et al., 2009; Hilvo et al, 2008). The sixteen isozymes differ in their subcellular localization, catalytic activity and susceptibility to different classes of inhibitors. Some of them are cytosolic (CA I, CA II, CA III, CA VII and CA XIII), others are membrane bound (CA IV, CA IX, CA XII and CA XIV), two are mitochondrial (CA VA and CA VB), and one is secreted in saliva (CA VI). It has been reported that CA XV isoform is not expressed in humans or in other primates, but it is abundant in rodents and other vertebrates (Table 1.) (Nair et al., 1994; Parkkila et al., 1996; Pastorekava et al., 2004; Bayram et al., 2008; Innocenti et al., 2008a,b; Senturk et al., 2009; Ekinci et al., 2011). CAs are produced in a variety of tissues where they participate in several important biological processes such as acid-base balance, respiration, carbon dioxide and ion transport, bone resorption, ureagenesis, gluconeogenesis, lipogenesis and body fluid generation (Supuran, 2008a,b,c). CA isozymes involved in these processes are important therapeutic targets with the potential to be inhibited / activated for the treatment of a range of disorders such as edema, glaucoma, obesity, cancer, epilepsy and osteoporosis (Innocenti et al., 2008b; Ekinci et al., 2007; Ekinci et al., 2011).

Carbonic Anhydrase Inhibitors and Activators: Small Organic Molecules as Drugs and Prodrugs