Inhibition of proteolysis and other posttranslational modifications with substrate-targeted inhibitors.
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.
D001665:Binding Sites; D010450:Endopeptidases / Q000737:chemistry / Q000378:metabolism; D011480:Protease Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011487:Protein Conformation; D017368:Protein Prenylation; D011499:Protein Processing, Post-Translational
D011480:Protease Inhibitors; D010450:Endopeptidases