Mapping the S1 and S1' subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents.

• Egile Nagusiak: Lorenzo Cianni (Egilea), Carina Lemke (Egilea), Erik Gilberg (Egilea), Christian Feldmann (Egilea), Fabiana Rosini (Egilea), Fernanda Dos Reis Rocho (Egilea), Jean F R Ribeiro (Egilea), Daiane Y Tezuka (Egilea), Carla D Lopes (Egilea), Sérgio de Albuquerque (Egilea), Jürgen Bajorath (Egilea), Stefan Laufer (Egilea), Andrei Leitão (Egilea), Michael Gütschow (Egilea), Carlos A Montanari (Egilea)
• Formatua: Liburua
• Argitaratua: Public Library of Science (PLoS), 2020-03-01T00:00:00Z.
• Gaiak: article
• Sarrera elektronikoa: Connect to this object online.

The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. A series of 26 new compounds were designed, synthesized, and tested against the recombinant cruzain (Cz) to map its S1/S1´ subsites. The same series was evaluated o...