William R. Roush, Alejandro Alvarez Hernández, James H. McKerrow, Paul M. Selzer, Elizabeth Hansell and Juan C. Engel. Design, Synthesis and Evaluation of D-Homophenylalanyl Epoxysuccinate Inhibitors of the Trypanosomal Cysteine Protease Cruzain. Tetrahedron, 2000, 56, 9747-9762. ISNN 0040-40200563-2064. Pergamon Press New York, Estados Unidos de America.
The binding modes of E-64c to papain combined with molecular modeling and ligand design using the crystal structure of cruzain have been used to develop new, potent d-Homophenylalanyl epoxysuccinate inhibitors of cruzain, the major cysteine protease of Trypanosoma cruzi. The most potent inhibitor 47 contains an O-benzyl hydroxamate unit and is highly specific for cruzain relative to other cysteine proteases tested.