Abstract
In single domain, “standard mechanism” protein inhibitors of serine proteinases, about a dozen residues make contact with the cognate enzyme. The remainder of the molecule, the scaffolding, holds the reactive site region of the inhibitor in a canonical conformation, improves the binding by about six orders of magnitude and protects it from proteolysis. However, the stability and global structure of the scaffolding is irrelevant to inhibition, provided that inhibition is measured much below the melting temperature,™.
Keywords: standard mechanism inhibitors, scaffolding, serine proteinases, inhibitor stability
Protein & Peptide Letters
Title: The Role of Scaffolding in Standard Mechanism Serine Proteinase Inhibitors
Volume: 12 Issue: 5
Author(s): Clyde A. Kelly, Michael Laskowski Jr. and M. A. Qasim
Affiliation:
Keywords: standard mechanism inhibitors, scaffolding, serine proteinases, inhibitor stability
Abstract: In single domain, “standard mechanism” protein inhibitors of serine proteinases, about a dozen residues make contact with the cognate enzyme. The remainder of the molecule, the scaffolding, holds the reactive site region of the inhibitor in a canonical conformation, improves the binding by about six orders of magnitude and protects it from proteolysis. However, the stability and global structure of the scaffolding is irrelevant to inhibition, provided that inhibition is measured much below the melting temperature,™.
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Cite this article as:
Kelly A. Clyde, Laskowski Jr. Michael and Qasim A. M., The Role of Scaffolding in Standard Mechanism Serine Proteinase Inhibitors, Protein & Peptide Letters 2005; 12 (5) . https://dx.doi.org/10.2174/0929866054395383
DOI https://dx.doi.org/10.2174/0929866054395383 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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