*** IBB - CNR *** Consiglio Nazionale delle Ricerche - Istituto di Biostrutture e Bioimmagini Naples. Italy., Neurofarba Department, Section of Pharmaceutical and Nutraceutical Sciences, Universita degli Studi di Firenze, Sesto Fiorentino, Florence. Italy.,
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 188.8.131.52) 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 -CA class, L. donovani chagasi for a beta-CA (LdcCA), whereas T. cruzi genome contains an alpha-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.
29 Records (29 escludendo Abstract e Conferenze). Impact factor totale: 174.701 (174.701 escludendo Abstract e Conferenze). Impact factor a 5 anni totale: 171.655 (171.655 escludendo Abstract e Conferenze).