A Computational Pipeline Observes the Flexibility and Dynamics of Plant Cytochrome P450 Binding Sites

Binding site flexibility and dynamics strongly affect the ability of proteins to accommodate substrates and inhibitors. The significance of these properties is particularly pronounced for proteins that are inherently flexible, such as cytochrome P450 enzymes (CYPs). While the research on human CYPs provides detailed knowledge on both structural and functional level, such analyses are still lacking for their plant counterparts. This study aims to bridge this gap. We developed a novel computational pipeline consisting of two steps. Firstly, we use molecular dynamics (MD) simulations to capture the full conformational ensemble for a certain plant CYP. Subsequently, we developed and applied a comprehensive methodology to analyze a number of binding site properties-size, flexibility, shape, hydrophobicity, and accessibility-using the fpocket and mdpocket packages on MD-generated trajectories. The workflow was validated on human CYPs 1A2, 2A6, and 3A4, as their binding site characteristics are well known. Not only could we confirm known binding site properties, but we also identified and named previously unseen binding site channels for CYPs 1A2 and 2A6. The pipeline was then applied to plant CYPs, leading to the first categorization of 15 chosen plant CYPs based on their binding site's (dis)similarities. This study provides a foundation for the largely uncharted fields of plant CYP substrate specificity and facilitates a more precise understanding of their largely unknown specific biological functions. It offers new insights into the structural and functional dynamics of plant CYPs, which may facilitate a more accurate understanding of the fate of agrochemicals or the biotechnological design and exploitation of enzymes with specific functions. Additionally, it serves as a reference for future structural-functional analyses of CYP enzymes across various biological kingdoms.

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Publication Details

Journal
International Journal of Molecular Sciences
Published
2024-10-23
DOI
https://doi.org/10.3390/ijms252111381
Citations
2
Primary Topic
Pharmacogenetics and Drug Metabolism
Type
article
Field-Weighted Citation Impact
0.93

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article

A Computational Pipeline Observes the Flexibility and Dynamics of Plant Cytochrome P450 Binding Sites

Anna Berteotti, Chris Oostenbrink, Klaus‐Jürgen Schleifer, Tea Kuvek et al.
2 citations
International Journal of Molecular Sciences
Pharmacogenetics and Drug Metabolism
0.93
article

A Computational Pipeline Observes the Flexibility and Dynamics of Plant Cytochrome P450 Binding Sites

Anna Berteotti, Chris Oostenbrink, Klaus‐Jürgen Schleifer, Tea Kuvek, Claudia Marcher, Veronica Lopez Carrillo
article en
2 citations

Abstract

Binding site flexibility and dynamics strongly affect the ability of proteins to accommodate substrates and inhibitors. The significance of these properties is particularly pronounced for proteins that are inherently flexible, such as cytochrome P450 enzymes (CYPs). While the research on human CYPs provides detailed knowledge on both structural and functional level, such analyses are still lacking for their plant counterparts. This study aims to bridge this gap. We developed a novel computational pipeline consisting of two steps. Firstly, we use molecular dynamics (MD) simulations to capture the full conformational ensemble for a certain plant CYP. Subsequently, we developed and applied a comprehensive methodology to analyze a number of binding site properties-size, flexibility, shape, hydrophobicity, and accessibility-using the fpocket and mdpocket packages on MD-generated trajectories. The workflow was validated on human CYPs 1A2, 2A6, and 3A4, as their binding site characteristics are well known. Not only could we confirm known binding site properties, but we also identified and named previously unseen binding site channels for CYPs 1A2 and 2A6. The pipeline was then applied to plant CYPs, leading to the first categorization of 15 chosen plant CYPs based on their binding site's (dis)similarities. This study provides a foundation for the largely uncharted fields of plant CYP substrate specificity and facilitates a more precise understanding of their largely unknown specific biological functions. It offers new insights into the structural and functional dynamics of plant CYPs, which may facilitate a more accurate understanding of the fate of agrochemicals or the biotechnological design and exploitation of enzymes with specific functions. Additionally, it serves as a reference for future structural-functional analyses of CYP enzymes across various biological kingdoms.

International Journal of Molecular SciencesVol. 25(21)
Christian Doppler Laboratory for Thermoelectricity (AT), Robert Bosch (Germany) (DE), BOKU University (AT)
Österreichische Nationalstiftung für Forschung, Technologie und Entwicklung, Austrian Science Fund, Christian Doppler Forschungsgesellschaft, Bundesministerium für Digitalisierung und Wirtschaftsstandort
Openalex Percentile: Top 24%
Pharmacogenetics and Drug Metabolism
0.93
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