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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...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BioMed Central
2016
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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. |
format | Online Article Text |
id | pubmed-4994241 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
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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