碳酸氢酶是对抗原生动物寄生虫病的合适靶点吗？

Title:Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases?

Volume: 25 Issue: 39

关键词: 碳酸酐酶，寄生虫病，疟疾，利什曼病，南美锥虫病，原生动物

摘要: 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.

Cite this article as:

Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases?, Current Medicinal Chemistry 2018; 25 (39) . https://dx.doi.org/10.2174/0929867325666180326160121