Figure 1.

Structures of representative irreversible β5i selective inhibitors and schematic for β-amino acid based noncovalent N,C-capped peptidomimetics. A) Peptide epoxyketones; B) Peptide sulfonyl fluoride; C) β5i Cys48 reacting N,C-capped peptides; D) 1,3,4-oxathiazol-2-ones; E) Schematic for conversion of N,C-capped dipeptides to β-amino acid-based dipeptidomimetics. N- and C- caps bind to S4 and S1 pockets of the β5, respectively. P1 binds to S2 and P2 binds to S3.