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Evaluation of a novel virtual screening strategy using receptor decoy binding sites

Virtual screening is used in biomedical research to predict the binding affinity of a large set of small organic molecules to protein receptor targets. This report shows the development and evaluation of a novel yet straightforward attempt to improve this ranking in receptor-based molecular docking...

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Autores principales: Patel, Hershna, Kukol, Andreas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4994241/
https://www.ncbi.nlm.nih.gov/pubmed/27553084
http://dx.doi.org/10.1186/s12952-016-0058-8
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author Patel, Hershna
Kukol, Andreas
author_facet Patel, Hershna
Kukol, Andreas
author_sort Patel, Hershna
collection PubMed
description Virtual screening is used in biomedical research to predict the binding affinity of a large set of small organic molecules to protein receptor targets. This report shows the development and evaluation of a novel yet straightforward attempt to improve this ranking in receptor-based molecular docking using a receptor-decoy strategy. This strategy includes defining a decoy binding site on the receptor and adjusting the ranking of the true binding-site virtual screen based on the decoy-site screen. The results show that by docking against a receptor-decoy site with Autodock Vina, improved Receiver Operator Characteristic Enrichment (ROCE) was achieved for 5 out of fifteen receptor targets investigated, when up to 15 % of a decoy site rank list was considered. No improved enrichment was seen for 7 targets, while for 3 targets the ROCE was reduced. The extent to which this strategy can effectively improve ligand prediction is dependent on the target receptor investigated.
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spelling pubmed-49942412016-08-24 Evaluation of a novel virtual screening strategy using receptor decoy binding sites Patel, Hershna Kukol, Andreas J Negat Results Biomed Brief Report Virtual screening is used in biomedical research to predict the binding affinity of a large set of small organic molecules to protein receptor targets. This report shows the development and evaluation of a novel yet straightforward attempt to improve this ranking in receptor-based molecular docking using a receptor-decoy strategy. This strategy includes defining a decoy binding site on the receptor and adjusting the ranking of the true binding-site virtual screen based on the decoy-site screen. The results show that by docking against a receptor-decoy site with Autodock Vina, improved Receiver Operator Characteristic Enrichment (ROCE) was achieved for 5 out of fifteen receptor targets investigated, when up to 15 % of a decoy site rank list was considered. No improved enrichment was seen for 7 targets, while for 3 targets the ROCE was reduced. The extent to which this strategy can effectively improve ligand prediction is dependent on the target receptor investigated. BioMed Central 2016-08-23 /pmc/articles/PMC4994241/ /pubmed/27553084 http://dx.doi.org/10.1186/s12952-016-0058-8 Text en © The Author(s). 2016 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Brief Report
Patel, Hershna
Kukol, Andreas
Evaluation of a novel virtual screening strategy using receptor decoy binding sites
title Evaluation of a novel virtual screening strategy using receptor decoy binding sites
title_full Evaluation of a novel virtual screening strategy using receptor decoy binding sites
title_fullStr Evaluation of a novel virtual screening strategy using receptor decoy binding sites
title_full_unstemmed Evaluation of a novel virtual screening strategy using receptor decoy binding sites
title_short Evaluation of a novel virtual screening strategy using receptor decoy binding sites
title_sort evaluation of a novel virtual screening strategy using receptor decoy binding sites
topic Brief Report
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4994241/
https://www.ncbi.nlm.nih.gov/pubmed/27553084
http://dx.doi.org/10.1186/s12952-016-0058-8
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