Virtual Double-System Single-Box for Absolute Dissociation Free Energy Calculations in GROMACS.


Journal

Journal of chemical information and modeling
ISSN: 1549-960X
Titre abrégé: J Chem Inf Model
Pays: United States
ID NLM: 101230060

Informations de publication

Date de publication:
22 11 2021
Historique:
pubmed: 2 11 2021
medline: 25 11 2021
entrez: 1 11 2021
Statut: ppublish

Résumé

We describe a step-by-step protocol for the computation of absolute dissociation free energy with GROMACS code and PLUMED library, which exploits a combination of advanced sampling techniques and nonequilibrium alchemical methodologies. The computational protocol has been automated through an open source Python middleware (HPC_Drug) which allows one to set up the GROMACS/PLUMED input files for execution on high performing computing facilities. The proposed protocol, by exploiting its inherent parallelism and the power of the GROMACS code on graphical processing units, has the potential to afford accurate and precise estimates of the dissociation constants in drug-receptor systems described at the atomistic level. The procedure has been applied to the calculation of the absolute dissociation free energy of PF-07321332, an oral antiviral proposed by Pfizer, with the main protease (3CL

Identifiants

pubmed: 34723516
doi: 10.1021/acs.jcim.1c00909
pmc: PMC8611716
doi:

Substances chimiques

Antiviral Agents 0
Lactams 0
Nitriles 0
nirmatrelvir 7R9A5P7H32
Proline 9DLQ4CIU6V
Leucine GMW67QNF9C

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

5320-5326

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Auteurs

Marina Macchiagodena (M)

Dipartimento di Chimica "Ugo Schiff", Università degli Studi di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.

Maurice Karrenbrock (M)

Dipartimento di Chimica "Ugo Schiff", Università degli Studi di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.

Marco Pagliai (M)

Dipartimento di Chimica "Ugo Schiff", Università degli Studi di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.

Piero Procacci (P)

Dipartimento di Chimica "Ugo Schiff", Università degli Studi di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy.

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Classifications MeSH