Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0

Abstract Background Network generation tools coupled with chemical reaction rules have been mainly developed for synthesis planning and more recently for metabolic engineering. Using the same core algorithm, these tools apply a set of rules to a source set of compounds, stopping when a sink set of c...

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Main Authors: Mathilde Koch, Thomas Duigou, Pablo Carbonell, Jean-Loup Faulon
Format: Article
Language:English
Published: BMC 2017-12-01
Series:Journal of Cheminformatics
Subjects:
Online Access:http://link.springer.com/article/10.1186/s13321-017-0252-9
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author Mathilde Koch
Thomas Duigou
Pablo Carbonell
Jean-Loup Faulon
author_facet Mathilde Koch
Thomas Duigou
Pablo Carbonell
Jean-Loup Faulon
author_sort Mathilde Koch
collection DOAJ
description Abstract Background Network generation tools coupled with chemical reaction rules have been mainly developed for synthesis planning and more recently for metabolic engineering. Using the same core algorithm, these tools apply a set of rules to a source set of compounds, stopping when a sink set of compounds has been produced. When using the appropriate sink, source and rules, this core algorithm can be used for a variety of applications beyond those it has been developed for. Results Here, we showcase the use of the open source workflow RetroPath2.0. First, we mathematically prove that we can generate all structural isomers of a molecule using a reduced set of reaction rules. We then use this enumeration strategy to screen the chemical space around a set of monomers and predict their glass transition temperatures, as well as around aminoglycosides to search structures maximizing antibacterial activity. We also perform a screening around aminoglycosides with enzymatic reaction rules to ensure biosynthetic accessibility. We finally use our workflow on an E. coli model to complete E. coli metabolome, with novel molecules generated using promiscuous enzymatic reaction rules. These novel molecules are searched on the MS spectra of an E. coli cell lysate interfacing our workflow with OpenMS through the KNIME Analytics Platform. Conclusion We provide an easy to use and modify, modular, and open-source workflow. We demonstrate its versatility through a variety of use cases including molecular structure enumeration, virtual screening in the chemical space, and metabolome completion. Because it is open source and freely available on MyExperiment.org, workflow community contributions should likely expand further the features of the tool, even beyond the use cases presented in the paper.
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spelling doaj.art-05ed55beac6d46c4872de25236c9915d2022-12-22T01:16:00ZengBMCJournal of Cheminformatics1758-29462017-12-019111710.1186/s13321-017-0252-9Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0Mathilde Koch0Thomas Duigou1Pablo Carbonell2Jean-Loup Faulon3Micalis Institute, INRA, AgroParisTech, Université Paris-SaclayMicalis Institute, INRA, AgroParisTech, Université Paris-SaclaySYNBIOCHEM Centre, Manchester Institute of Biotechnology, University of ManchesterMicalis Institute, INRA, AgroParisTech, Université Paris-SaclayAbstract Background Network generation tools coupled with chemical reaction rules have been mainly developed for synthesis planning and more recently for metabolic engineering. Using the same core algorithm, these tools apply a set of rules to a source set of compounds, stopping when a sink set of compounds has been produced. When using the appropriate sink, source and rules, this core algorithm can be used for a variety of applications beyond those it has been developed for. Results Here, we showcase the use of the open source workflow RetroPath2.0. First, we mathematically prove that we can generate all structural isomers of a molecule using a reduced set of reaction rules. We then use this enumeration strategy to screen the chemical space around a set of monomers and predict their glass transition temperatures, as well as around aminoglycosides to search structures maximizing antibacterial activity. We also perform a screening around aminoglycosides with enzymatic reaction rules to ensure biosynthetic accessibility. We finally use our workflow on an E. coli model to complete E. coli metabolome, with novel molecules generated using promiscuous enzymatic reaction rules. These novel molecules are searched on the MS spectra of an E. coli cell lysate interfacing our workflow with OpenMS through the KNIME Analytics Platform. Conclusion We provide an easy to use and modify, modular, and open-source workflow. We demonstrate its versatility through a variety of use cases including molecular structure enumeration, virtual screening in the chemical space, and metabolome completion. Because it is open source and freely available on MyExperiment.org, workflow community contributions should likely expand further the features of the tool, even beyond the use cases presented in the paper.http://link.springer.com/article/10.1186/s13321-017-0252-9Scientific workflowsChemical spaceReaction networks generationRetrosynthesisReaction rulesIsomer enumeration
spellingShingle Mathilde Koch
Thomas Duigou
Pablo Carbonell
Jean-Loup Faulon
Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0
Journal of Cheminformatics
Scientific workflows
Chemical space
Reaction networks generation
Retrosynthesis
Reaction rules
Isomer enumeration
title Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0
title_full Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0
title_fullStr Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0
title_full_unstemmed Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0
title_short Molecular structures enumeration and virtual screening in the chemical space with RetroPath2.0
title_sort molecular structures enumeration and virtual screening in the chemical space with retropath2 0
topic Scientific workflows
Chemical space
Reaction networks generation
Retrosynthesis
Reaction rules
Isomer enumeration
url http://link.springer.com/article/10.1186/s13321-017-0252-9
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