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Multiscale Ensemble Computing for Modelling Biological Catalysts

Lead Research Organisation: University of Bristol
Department Name: Chemistry

Abstract

The goal of this project is to use the flexible HPC resource made available on HPCx to perform a detailed investigation of the mechanism of chemical reactions catalysed by the enzyme fatty acid amide hydrolase (FAAH), an important target for drug development. HPC resources are increasingly helping to illuminate and analyse the fundamental mechanisms of biological 'molecular machines'. An example is enzyme catalysis. Enzymes are very efficient natural catalysts. Understanding how they work is a vital first step to the goal of harnessing their power for industrial and pharmaceutical applications. For example, many drugs work by stopping enzymes from functioning.Atomically detailed computer models of enzyme-catalysed reactions provide an insight into the source of an enzyme's power. Due to the large size of biological molecules, simplified classical models of atomic interactions are used. These molecular mechanics (MM) models have been used successfully to understand the molecular dynamics of proteins. However, MM can provide only a low-quality model of a chemical reaction, as electrons are represented implicitly. The best quality chemical models are provided by quantum mechanics (QM). QM calculations are highly computationally expensive, so it would be challenging to solve a QM model of an entire enzyme system. One solution is to use multiscale methods that embed a QM representation of the reactive region of the enzyme within an MM model of the rest of the system. Multilevel simulations of biological systems scale poorly over the many processors available on an HPC resource. New multiscale modelling methods(4) that split a single calculation into an ensemble of loosely-coupled simulations, are therefore a promising new direction to utilize maximum computingpower. The aim is to make best use of the large numbers of processors by effectively coupling multiple individual simulations into a single supra-simulation. This method, applied on an HPC resource, promises to lead to a step change in the quality of the modelling of enzyme-catalysed reactions, and will provide new insights into these remarkable biological molecules.

Publications

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McGeagh JD (2011) Protein dynamics and enzyme catalysis: insights from simulations. in Biochimica et biophysica acta

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Meletiou A (2019) Tios: The Internet of Simulations. Turning Molecular Dynamics into a Data Streaming Web Application. in Journal of chemical information and modeling

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Minguez Teresa (2020) Novel determinants of agonist selectivity in nicotinic ACh receptors in BRITISH JOURNAL OF PHARMACOLOGY

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Motta S (2018) Ligand-induced perturbation of the HIF-2a:ARNT dimer dynamics. in PLoS computational biology

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Mujika JI (2009) Modeling protein splicing: reaction pathway for C-terminal splice and intein scission. in The journal of physical chemistry. B

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Mulholland A (1998) A model of the condensation step in the citrate synthase reaction in Journal of Molecular Structure: THEOCHEM

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Mulholland A (2012) Enzyme dynamics and catalysis in the mechanism of DNA polymerase in Theoretical Chemistry Accounts

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Mulholland A (2020) Letter to the Editor. in Journal of paediatrics and child health

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Mulholland A (1998) Calculations on the substrates of citrate synthase I. Oxaloacetate in Journal of Molecular Structure: THEOCHEM

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Mulholland Adrian J. (2009) PHYS 47-Biomolecular simulations of enzymatic reactions in ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY

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Mulholland AJ (1996) Simulations of enzymic reactions. in Biochemical Society transactions

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Mulholland AJ (2023) Science after Brexit: bright spots on the Horizon? in EMBO reports

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Mulholland AJ (2020) COVID19 - Computational Chemists Meet the Moment. in Journal of chemical information and modeling

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Mulholland AJ (2016) Dispelling the effects of a sorceress in enzyme catalysis. in Proceedings of the National Academy of Sciences of the United States of America

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Musgaard M (2016) Steered Molecular Dynamics Simulations Predict Conformational Stability of Glutamate Receptors. in Journal of chemical information and modeling

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Nesabi A (2024) Molecular dynamics simulations as a guide for modulating small molecule aggregation. in Journal of computer-aided molecular design

 
Description BBSRC Tools and Techniques: Computational tools for enzyme engineering: bridging the gap between enzymologists and expert simulation
Amount £146,027 (GBP)
Funding ID BB/L018756/1 
Organisation Biotechnology and Biological Sciences Research Council (BBSRC) 
Sector Public
Country United Kingdom
Start 06/2014 
End 01/2016
 
Description Biocatalysis and Biotransformation: A 5th Theme for the National Catalysis Hub
Amount £3,053,639 (GBP)
Funding ID EP/M013219/1 
Organisation Engineering and Physical Sciences Research Council (EPSRC) 
Sector Public
Country United Kingdom
Start 01/2015 
End 12/2019
 
Title Sire 2009.1 
Description 2009.1 release of the Sire molecular simulation framework. Main enhancement was making the code portable to a wide range of architectures, e.g. including PowerPC/AIX (so that the code could run efficiently on HPCx) and enhancing the functionality of the QM/MM free energy code. 
Type Of Technology Software 
Year Produced 2009 
Open Source License? Yes  
Impact Sire is used in several pharmaceutical companies for applications in drug design and development. This version of the code was used to run the simulations in "Compatibility of Quantum Chemical Methods and Empirical (MM) Water Models in Quantum Mechanics / Molecular Mechanics Liquid Water Simulations", J. Phys. Chem. Lett., doi:10.1021/jz900096p and "Combined Quantum Mechanics Molecular Mechanics (QM MM) Simulations for Protein Ligand Complexes: Free Energies of Binding of Water Molecules in Influenza Neuraminidase", J. Phys. Chem. B, 2014, Accepted 10.1021/jp506413j 
URL http://www.siremol.org/Sire/Home.html