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

• Main Authors: Lorenzo Cianni (Author), Carina Lemke (Author), Erik Gilberg (Author), Christian Feldmann (Author), Fabiana Rosini (Author), Fernanda Dos Reis Rocho (Author), Jean F R Ribeiro (Author), Daiane Y Tezuka (Author), Carla D Lopes (Author), Sérgio de Albuquerque (Author), Jürgen Bajorath (Author), Stefan Laufer (Author), Andrei Leitão (Author), Michael Gütschow (Author), Carlos A Montanari (Author)
• Format: Book
• Published: Public Library of Science (PLoS), 2020-03-01T00:00:00Z.
• Subjects: article
• Online Access: 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...