Large scale relative protein ligand binding affinities using non-equilibrium alchemy

V Gapsys, L Pérez-Benito, M Aldeghi, D Seeliger… - Chemical …, 2020 - pubs.rsc.org
Ligand binding affinity calculations based on molecular dynamics (MD) simulations and non-
physical (alchemical) thermodynamic cycles have shown great promise for structure-based …

Advances in the calculation of binding free energies

A de Ruiter, C Oostenbrink - Current opinion in structural biology, 2020 - Elsevier
Highlights•Binding free energy calculations are increasing used in drug design and
biotechnology.•We distinguish end-state methods, alchemical methods and pathway …

Computational studies of protein–drug binding affinity changes upon mutations in the drug target

R Friedman - Wiley Interdisciplinary Reviews: Computational …, 2022 - Wiley Online Library
Mutations that lead to drug resistance limit the efficacy of antibiotics, antiviral drugs, targeted
cancer therapies, and other treatments. Accurately calculating protein–drug binding affinity …

Evolution of alchemical free energy methods in drug discovery

LF Song, KM Merz Jr - Journal of Chemical Information and …, 2020 - ACS Publications
The goal of the present manuscript is to succinctly trace the key technological steps in the
evolution of alchemical free energy methods (AFEMs) from a purely theoretical construct to a …

Dimerization of the deaminase domain and locking interactions with Cas9 boost base editing efficiency in ABE8e

PR Arantes, X Chen, S Sinha, A Saha… - Nucleic acids …, 2024 - academic.oup.com
CRISPR-based DNA adenine base editors (ABEs) hold remarkable promises to address
human genetic diseases caused by point mutations. ABEs were developed by combining …

SAMPL7 Host–Guest Challenge Overview: assessing the reliability of polarizable and non-polarizable methods for binding free energy calculations

M Amezcua, L El Khoury, DL Mobley - Journal of computer-aided …, 2021 - Springer
The SAMPL challenges focus on testing and driving progress of computational methods to
help guide pharmaceutical drug discovery. However, assessment of methods for predicting …

Pre‐exascale HPC approaches for molecular dynamics simulations. Covid‐19 research: A use case

M Wieczor, V Genna, J Aranda… - Wiley …, 2023 - Wiley Online Library
Exascale computing has been a dream for ages and is close to becoming a reality that will
impact how molecular simulations are being performed, as well as the quantity and quality of …

Comparing Supervised Learning and Rigorous Approach for Predicting Protein Stability upon Point Mutations in Difficult Targets

J Kurniawan, T Ishida - Journal of Chemical Information and …, 2023 - ACS Publications
Accurate prediction of protein stability upon a point mutation has important applications in
drug discovery and personalized medicine. It remains a challenging issue in computational …

Methodological uncertainties in drug-receptor binding free energy predictions based on classical molecular dynamics

P Procacci - Current Opinion in Structural Biology, 2021 - Elsevier
Highlights•Computational approaches are becoming an essential tool in modern drug
design.•Development of automated workflows from docking to MD techniques for drug …

QresFEP: an automated protocol for free energy calculations of protein mutations in Q

W Jespers, GV Isaksen, TAH Andberg… - Journal of Chemical …, 2019 - ACS Publications
Predicting the effect of single-point mutations on protein stability or protein–ligand binding is
a major challenge in computational biology. Free energy calculations constitute the most …