Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase

© 2017 Wiley Periodicals, Inc. Cholesterol oxidase (ChOx) is a flavoenzyme that oxidizes and isomerizes cholesterol (CHL) to form cholest-4-en-3-one. Molecular docking and molecular dynamics simulations were conducted to predict the binding interactions of CHL in the active site. Several key intera...

Full description

Bibliographic Details
Main Authors: Harb, L., Arooj, Mahreen, Vrielink, A., Mancera, Ricardo
Format: Journal Article
Published: John Wiley & Sons, Inc. 2017
Online Access:http://hdl.handle.net/20.500.11937/63291
_version_ 1848761047039606784
author Harb, L.
Arooj, Mahreen
Vrielink, A.
Mancera, Ricardo
author_facet Harb, L.
Arooj, Mahreen
Vrielink, A.
Mancera, Ricardo
author_sort Harb, L.
building Curtin Institutional Repository
collection Online Access
description © 2017 Wiley Periodicals, Inc. Cholesterol oxidase (ChOx) is a flavoenzyme that oxidizes and isomerizes cholesterol (CHL) to form cholest-4-en-3-one. Molecular docking and molecular dynamics simulations were conducted to predict the binding interactions of CHL in the active site. Several key interactions (E361-CHL, N485-FAD, and H447-CHL) were identified and which are likely to determine the correct positioning of CHL relative to flavin-adenine dinucleotide (FAD). Binding of CHL also induced changes in key residues of the active site leading to the closure of the oxygen channel. A group of residues, Y107, F444, and Y446, known as the hydrophobic triad, are believed to affect the binding of CHL in the active site. Computational site-directed mutagenesis of these residues revealed that their mutation affects the conformations of key residues in the active site, leading to non-optimal binding of CHL and to changes in the structure of the oxygen channel, all of which are likely to reduce the catalytic efficiency of ChOx. Proteins 2017; 85:1645–1655. © 2017 Wiley Periodicals, Inc.
first_indexed 2025-11-14T10:25:27Z
format Journal Article
id curtin-20.500.11937-63291
institution Curtin University Malaysia
institution_category Local University
last_indexed 2025-11-14T10:25:27Z
publishDate 2017
publisher John Wiley & Sons, Inc.
recordtype eprints
repository_type Digital Repository
spelling curtin-20.500.11937-632912018-02-06T06:24:17Z Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase Harb, L. Arooj, Mahreen Vrielink, A. Mancera, Ricardo © 2017 Wiley Periodicals, Inc. Cholesterol oxidase (ChOx) is a flavoenzyme that oxidizes and isomerizes cholesterol (CHL) to form cholest-4-en-3-one. Molecular docking and molecular dynamics simulations were conducted to predict the binding interactions of CHL in the active site. Several key interactions (E361-CHL, N485-FAD, and H447-CHL) were identified and which are likely to determine the correct positioning of CHL relative to flavin-adenine dinucleotide (FAD). Binding of CHL also induced changes in key residues of the active site leading to the closure of the oxygen channel. A group of residues, Y107, F444, and Y446, known as the hydrophobic triad, are believed to affect the binding of CHL in the active site. Computational site-directed mutagenesis of these residues revealed that their mutation affects the conformations of key residues in the active site, leading to non-optimal binding of CHL and to changes in the structure of the oxygen channel, all of which are likely to reduce the catalytic efficiency of ChOx. Proteins 2017; 85:1645–1655. © 2017 Wiley Periodicals, Inc. 2017 Journal Article http://hdl.handle.net/20.500.11937/63291 10.1002/prot.25319 John Wiley & Sons, Inc. restricted
spellingShingle Harb, L.
Arooj, Mahreen
Vrielink, A.
Mancera, Ricardo
Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
title Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
title_full Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
title_fullStr Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
title_full_unstemmed Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
title_short Computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
title_sort computational site-directed mutagenesis studies of the role of the hydrophobic triad on substrate binding in cholesterol oxidase
url http://hdl.handle.net/20.500.11937/63291