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@ARTICLE{DeVivo:820516,
author = {De Vivo, Marco and Masetti, Matteo and Bottegoni, Giovanni
and Cavalli, Andrea},
title = {{R}ole of {M}olecular {D}ynamics and {R}elated {M}ethods in
{D}rug {D}iscovery},
journal = {Journal of medicinal chemistry},
volume = {59},
number = {9},
issn = {1520-4804},
address = {Washington, DC},
publisher = {ACS},
reportid = {FZJ-2016-05808},
pages = {4035 - 4061},
year = {2016},
abstract = {Molecular dynamics (MD) and related methods are close to
becoming routine computational tools for drug discovery.
Their main advantage is in explicitly treating structural
flexibility and entropic effects. This allows a more
accurate estimate of the thermodynamics and kinetics
associated with drug–target recognition and binding, as
better algorithms and hardware architectures increase their
use. Here, we review the theoretical background of MD and
enhanced sampling methods, focusing on free-energy
perturbation, metadynamics, steered MD, and other methods
most consistently used to study drug–target binding. We
discuss unbiased MD simulations that nowadays allow the
observation of unsupervised ligand–target binding,
assessing how these approaches help optimizing target
affinity and drug residence time toward improved drug
efficacy. Further issues discussed include allosteric
modulation and the role of water molecules in ligand binding
and optimization. We conclude by calling for more
prospective studies to attest to these methods’ utility in
discovering novel drug candidates.},
cin = {IAS-5 / INM-9},
ddc = {540},
cid = {I:(DE-Juel1)IAS-5-20120330 / I:(DE-Juel1)INM-9-20140121},
pnm = {899 - ohne Topic (POF3-899)},
pid = {G:(DE-HGF)POF3-899},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000375969200002},
pubmed = {pmid:26807648},
doi = {10.1021/acs.jmedchem.5b01684},
url = {https://juser.fz-juelich.de/record/820516},
}