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dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules

The development of open computational pipelines to accelerate the discovery of treatments for emerging diseases allows finding novel solutions in shorter periods of time. Consensus molecular docking is one of these approaches, and its main purpose is to increase the detection of real actives within...

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Autores principales: Ochoa, Rodrigo, Palacio-Rodriguez, Karen, Clemente, Camila M., Adler, Natalia S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Inc. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8442548/
https://www.ncbi.nlm.nih.gov/pubmed/34555725
http://dx.doi.org/10.1016/j.jmgm.2021.108023
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author Ochoa, Rodrigo
Palacio-Rodriguez, Karen
Clemente, Camila M.
Adler, Natalia S.
author_facet Ochoa, Rodrigo
Palacio-Rodriguez, Karen
Clemente, Camila M.
Adler, Natalia S.
author_sort Ochoa, Rodrigo
collection PubMed
description The development of open computational pipelines to accelerate the discovery of treatments for emerging diseases allows finding novel solutions in shorter periods of time. Consensus molecular docking is one of these approaches, and its main purpose is to increase the detection of real actives within virtual screening campaigns. Here we present dockECR, an open consensus docking and ranking protocol that implements the exponential consensus ranking method to prioritize molecular candidates. The protocol uses four open source molecular docking programs: AutoDock Vina, Smina, LeDock and rDock, to rank the molecules. In addition, we introduce a scoring strategy based on the average RMSD obtained from comparing the best poses from each single program to complement the consensus ranking with information about the predicted poses. The protocol was benchmarked using 15 relevant protein targets with known actives and decoys, and applied using the main protease of the SARS-CoV-2 virus. For the application, different crystal structures of the protease, and frames obtained from molecular dynamics simulations were used to dock a library of 79 molecules derived from previously co-crystallized fragments. The ranking obtained with dockECR was used to prioritize eight candidates, which were evaluated in terms of the interactions generated with key residues from the protease. The protocol can be implemented in any virtual screening campaign involving proteins as molecular targets. The dockECR code is publicly available at: https://github.com/rochoa85/dockECR.
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spelling pubmed-84425482021-09-15 dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules Ochoa, Rodrigo Palacio-Rodriguez, Karen Clemente, Camila M. Adler, Natalia S. J Mol Graph Model Article The development of open computational pipelines to accelerate the discovery of treatments for emerging diseases allows finding novel solutions in shorter periods of time. Consensus molecular docking is one of these approaches, and its main purpose is to increase the detection of real actives within virtual screening campaigns. Here we present dockECR, an open consensus docking and ranking protocol that implements the exponential consensus ranking method to prioritize molecular candidates. The protocol uses four open source molecular docking programs: AutoDock Vina, Smina, LeDock and rDock, to rank the molecules. In addition, we introduce a scoring strategy based on the average RMSD obtained from comparing the best poses from each single program to complement the consensus ranking with information about the predicted poses. The protocol was benchmarked using 15 relevant protein targets with known actives and decoys, and applied using the main protease of the SARS-CoV-2 virus. For the application, different crystal structures of the protease, and frames obtained from molecular dynamics simulations were used to dock a library of 79 molecules derived from previously co-crystallized fragments. The ranking obtained with dockECR was used to prioritize eight candidates, which were evaluated in terms of the interactions generated with key residues from the protease. The protocol can be implemented in any virtual screening campaign involving proteins as molecular targets. The dockECR code is publicly available at: https://github.com/rochoa85/dockECR. Elsevier Inc. 2021-12 2021-09-15 /pmc/articles/PMC8442548/ /pubmed/34555725 http://dx.doi.org/10.1016/j.jmgm.2021.108023 Text en © 2021 Elsevier Inc. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Ochoa, Rodrigo
Palacio-Rodriguez, Karen
Clemente, Camila M.
Adler, Natalia S.
dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules
title dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules
title_full dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules
title_fullStr dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules
title_full_unstemmed dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules
title_short dockECR: Open consensus docking and ranking protocol for virtual screening of small molecules
title_sort dockecr: open consensus docking and ranking protocol for virtual screening of small molecules
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8442548/
https://www.ncbi.nlm.nih.gov/pubmed/34555725
http://dx.doi.org/10.1016/j.jmgm.2021.108023
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