Abstract
Efficient binding of biomacromolecular surfaces by synthetic systems requires the effective presentation of complementary elements over large surface areas. We demonstrate here the use of mixed monolayer protected gold clusters (MMPCs) as scaffolds for the binding and inhibition of chymotrypsin. In these studies anionically functionalized amphiphilic MMPCs were shown to inhibit chymotrypsin through a two-stage mechanism featuring fast reversible inhibition followed by a slower irreversible process. This interaction is very efficient, with aK\documentclass[12pt]{minimal} \usepackage{amsmath} \usepackage{wasysym} \usepackage{amsfonts} \usepackage{amssymb} \usepackage{amsbsy} \usepackage{mathrsfs} \setlength{\oddsidemargin}{-69pt} \begin{document} \begin{equation*}{\mathrm{_{i}^{app}}}\end{equation*}\end{document}= 10.4 ± 1.3 nM. The MMPC–protein complex was characterized by CD, demonstrating an almost complete denaturation of the enzyme over time. Dynamic light scattering studies confirm that inhibition proceeds without substantial MMPC aggregation. The electrostatic nature of the engineered interactions provides a level of selectivity: little or no inhibition of function was observed with elastase, β-galactosidase, or cellular retinoic acid binding protein.
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Dates
Type | When |
---|---|
Created | 23 years, 1 month ago (July 26, 2002, 10:45 a.m.) |
Deposited | 1 year, 7 months ago (Jan. 3, 2024, 11:57 p.m.) |
Indexed | 2 days, 13 hours ago (Aug. 27, 2025, 11:46 a.m.) |
Issued | 23 years, 4 months ago (April 2, 2002) |
Published | 23 years, 4 months ago (April 2, 2002) |
Published Online | 23 years, 4 months ago (April 2, 2002) |
Published Print | 23 years, 4 months ago (April 16, 2002) |
@article{Fischer_2002, title={Inhibition of chymotrypsin through surface binding using nanoparticle-based receptors}, volume={99}, ISSN={1091-6490}, url={http://dx.doi.org/10.1073/pnas.082644099}, DOI={10.1073/pnas.082644099}, number={8}, journal={Proceedings of the National Academy of Sciences}, publisher={Proceedings of the National Academy of Sciences}, author={Fischer, Nicholas O. and McIntosh, Catherine M. and Simard, Joseph M. and Rotello, Vincent M.}, year={2002}, month=apr, pages={5018–5023} }