Title of article
Design, Synthesis and Evaluation of d-Homophenylalanyl Epoxysuccinate Inhibitors of the Trypanosomal Cysteine Protease Cruzain
Author/Authors
William R. Roush.، نويسنده , , Alejandro Alvarez-Hernandez، نويسنده , , James H McKerrow، نويسنده , , Paul M Selzer، نويسنده , , Elizabeth Hansell، نويسنده , , Juan C. Engel، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2000
Pages
16
From page
9747
To page
9762
Abstract
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.
Keywords
Enzyme inhibitors , hydroxamic acids and derivatives , peptide analogs and mimetics , Molecular design
Journal title
Tetrahedron
Serial Year
2000
Journal title
Tetrahedron
Record number
1081501
Link To Document