Substrate and inhibitor studies on proteinase 3
Open Access
- 3 February 1992
- journal article
- Published by Wiley in FEBS Letters
- Vol. 297 (1-2) , 119-123
- https://doi.org/10.1016/0014-5793(92)80340-m
Abstract
Various amino acid and peptide thioesters were tested as substrates for human proteinase 3 and the best substrate is Boc‐Ala‐Ala‐Nva‐SBzl with a k cal/K m value of 1.0 × 106nMit‐1sit‐1 Boc‐Ala‐Ala‐AA‐SBzl (AA = Val, Ala, or Met) are also good substrates with k cal/K m values of (1‐4) × 105 M−1 s−1. Substituted isocoumarins are potent inhibitors of proteinase 3 and the best inhibitors are 7‐amino‐4‐chloro‐3‐(2‐bromoethoxy)isocoumarin and 3.4‐dichloroisocoumarin (DCI) with k obs/[I] values of 4700 and 2600 M−1 s−1, respectively. Substituted isocoumarins. peptide phosphonates and chloromethyl ketones inhibited proteinase 3 less potently than human neutrophil elastase (HNE) by 1‐2 orders of magnitude.Keywords
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