Artículos de revistas
Identification of Levothyroxine Antichagasic Activity through Computer-Aided Drug Repurposing
Fecha
2014-01Registro en:
Bellera, Carolina Leticia; Balcazar, Dario Emmanuel; Alberca, Lucas Nicolás; Labriola, Carlos Alberto; Talevi, Alan; et al.; Identification of Levothyroxine Antichagasic Activity through Computer-Aided Drug Repurposing; Hindawi Publishing Corporation; The Scientific World Journal; 2014; 1-2014; 1-9
2356-6140
Autor
Bellera, Carolina Leticia
Balcazar, Dario Emmanuel
Alberca, Lucas Nicolás
Labriola, Carlos Alberto
Talevi, Alan
Carrillo, Carolina
Resumen
Cruzipain (Cz) is the major cysteine protease of the protozoan Trypanosoma cruzi, etiological agent of Chagas disease. A conformation-independent classifier capable of identifying Cz inhibitors was derived from a 163-compound dataset and later applied in a virtual screening campaign on the DrugBank database, which compiles FDA-approved and investigational drugs. 54 approved drugs were selected as candidates, 3 of which were acquired and tested on Cz and T. cruzi epimastigotes proliferation. Among them, levothyroxine, traditionally used in hormone replacement therapy in patients with hypothyroidism, showed dosedependent inhibition of Cz and antiproliferative activity on the parasite.