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Inhibition of proteolysis and other posttranslational modifications with substrate‐targeted inhibitors
Author(s) -
Kodadek Thomas
Publication year - 2002
Publication title -
peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/bip.10233
Subject(s) - proteolysis , proteases , chemistry , protease , substrate specificity , enzyme , substrate (aquarium) , biochemistry , epitope , combinatorial chemistry , biology , antigen , ecology , genetics
Abstract This article reviews the concept of developing protease inhibitors that target the substrate polypeptide rather than the enzyme. Substrate‐targeted inhibitors have the potential to be more specific than even the most highly selective enzyme‐targeted inhibitors because essentially all proteases process multiple substrates. The challenge in developing substrate‐targeted protease inhibitors centers on the development of high‐affinity binding agents for short stretches of amino acids (linear epitopes). Recent experimental progress toward this goal and a number of other potential solutions are discussed. © 2002 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 66: 134–140, 2002