Abstract
Protozoans belonging to Plasmodium, Leishmania and Trypanosoma genera provoke widespread parasitic diseases with few treatment options and many of the clinically used drugs experiencing an extensive drug resistance phenomenon. In the last several years, the metalloenzyme Carbonic Anhydrase (CA, EC 4.2.1.1) was cloned and characterized in the genome of these protozoa, with the aim to search for a new drug target for fighting malaria, leishmaniasis and Chagas disease. P. falciparum encodes for a CA (PfCA) belonging to a novel genetic family, the η-CA class, L. donovani chagasi for a β-CA (LdcCA), whereas T. cruzi genome contains an α-CA (TcCA). These three enzymes were characterized in detail and a number of in vitro potent and selective inhibitors belonging to the sulfonamide, thiol, dithiocarbamate and hydroxamate classes were discovered. Some of these inhibitors were also effective in cell cultures and animal models of protozoan infections, making them of considerable interest for the development of new antiprotozoan drugs with a novel mechanism of action.
Keywords: Carbonic anhydrases, parasitic diseases, malaria, leishmaniasis, Chagas disease, protozoa.
Current Medicinal Chemistry
Title:Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases?
Volume: 25 Issue: 39
Author(s): Katia D'Ambrosio*, Claudiu T. Supuran and Giuseppina De Simone*
Affiliation:
- Istituto di Biostrutture e Bioimmagini-CNR, Naples,Italy
- Istituto di Biostrutture e Bioimmagini-CNR, Naples,Italy
Keywords: Carbonic anhydrases, parasitic diseases, malaria, leishmaniasis, Chagas disease, protozoa.
Abstract: Protozoans belonging to Plasmodium, Leishmania and Trypanosoma genera provoke widespread parasitic diseases with few treatment options and many of the clinically used drugs experiencing an extensive drug resistance phenomenon. In the last several years, the metalloenzyme Carbonic Anhydrase (CA, EC 4.2.1.1) was cloned and characterized in the genome of these protozoa, with the aim to search for a new drug target for fighting malaria, leishmaniasis and Chagas disease. P. falciparum encodes for a CA (PfCA) belonging to a novel genetic family, the η-CA class, L. donovani chagasi for a β-CA (LdcCA), whereas T. cruzi genome contains an α-CA (TcCA). These three enzymes were characterized in detail and a number of in vitro potent and selective inhibitors belonging to the sulfonamide, thiol, dithiocarbamate and hydroxamate classes were discovered. Some of these inhibitors were also effective in cell cultures and animal models of protozoan infections, making them of considerable interest for the development of new antiprotozoan drugs with a novel mechanism of action.
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Cite this article as:
D'Ambrosio Katia *, Supuran T. Claudiu and De Simone Giuseppina *, Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases?, Current Medicinal Chemistry 2018; 25 (39) . https://dx.doi.org/10.2174/0929867325666180326160121
DOI https://dx.doi.org/10.2174/0929867325666180326160121 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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