Rational design of thioamide peptides as selective inhibitors of cysteine protease cathepsin L
Hoang Anh T. Phan, Sam Giannakoulias, Taylor M. Barrett, Chunxiao Liu, E. James Petersson
Abstract
= 19 μM). Our study demonstrates that one can rationally design a stabilized, specific peptidyl protease inhibitor by strategic placement of a thioamide and reaffirms the place of this single-atom modification in the toolbox of peptide-based rational drug design.
Topics & Concepts
ThioamideChemistryCathepsinCathepsin BCysteine proteaseCysteineRational designPeptideProteaseCathepsin LStereochemistryBiochemistryCombinatorial chemistryEnzymeBiologyGeneticsProtease and Inhibitor MechanismsOral microbiology and periodontitis researchAntimicrobial Peptides and Activities