Accuracy of Molecular Simulation-Based Predictions of k(off) Values: A Metadynamics Study
The k(off) values of ligands unbinding to proteins are key parameters for drug discovery. Their predictions based on molecular simulation may under- or overestimate experiment in a system- and/or technique-dependent way. Here we use an established method-infrequent metadynamics, based on the AMBER force field-to compute the k(off )of the ligand iperoxo (in clinical use) targeting the muscarinic receptor M-2. The ligand charges are calculated by either (i) the Amber standard procedure or (ii) B3LYP-DFT. The calculations using (i) turn out not to provide a reasonable estimation of the transition-state free energy. Those using (ii) differ from experiment by 2 orders of magnitude. On the basis of B3LYP DFT QM/MM simulations, we suggest that the observed discrepancy in (ii) arises, at least in part, from the lack of electronic polarization and/or charge transfer in biomolecular force fields. These issues might be present in other systems, such as DNA-protein complexes.
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Capelli, R., Lyu, W., Bolnykh, V., Meloni, S., Olsen, J. M. H., Rothlisberger, U., Parrinello, M., & Carloni, P. (2020). Accuracy of Molecular Simulation-Based Predictions of k(off) Values: A Metadynamics Study. The Journal of Physical Chemistry Letters, 11(15), 6373–6381. https://doi.org/10.1021/acs.jpclett.0c00999
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WOS:000562064500081
2020-08-06
11
15
6373
6381
REVIEWED
EPFL