Increased stability of peptidesulfonamide peptidomimetics towards protease catalyzed degradation.
Replacement of amide bonds in peptides by sulfonamide moieties resulted in peptidosulfonamides with an increased stability towards protease catalyzed degradation. In addition to protection of the protease cleavage site, it was found that introduction of a sulfonamide also influenced the stability of adjacent amide bonds.
de Bont
D B
DB
Department of Medicinal Chemistry, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, The Netherlands.
Sliedregt-Bol
K M
KM
Hofmeyer
L J
LJ
Liskamp
R M
RM
D001665:Binding Sites; D002384:Catalysis; D010450:Endopeptidases / Q000378:metabolism*; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D013379:Substrate Specificity; D013449:Sulfonamides / Q000737:chemistry / Q000378:metabolism*
D010455:Peptides; D013449:Sulfonamides; D010450:Endopeptidases