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@ARTICLE{Capelli:866015,
author = {Capelli, Riccardo and Bochicchio, Anna and Piccini,
GiovanniMaria and Casasnovas, Rodrigo and Carloni, Paolo and
Parrinello, Michele},
title = {{C}hasing the {F}ull {F}ree {E}nergy {L}andscape of
{N}euroreceptor/{L}igand {U}nbinding by {M}etadynamics
{S}imulations},
journal = {Journal of chemical theory and computation},
volume = {15},
number = {5},
issn = {1549-9626},
address = {Washington, DC},
reportid = {FZJ-2019-05275},
pages = {3354 - 3361},
year = {2019},
abstract = {Predicting the complete free energy landscape associated
with protein–ligand unbinding may greatly help designing
drugs with highly optimized pharmacokinetics. Here we
investigate the unbinding of the iperoxo agonist to its
target human neuroreceptor M2, embedded in a neuronal
membrane. By feeding out-of-equilibrium molecular
simulations data in a classification analysis, we identify
the few essential reaction coordinates of the process. The
full landscape is then reconstructed using an exact enhanced
sampling method, well-tempered metadynamics in its funnel
variant. The calculations reproduce well the measured
affinity, provide a rationale for mutagenesis data, and show
that the ligand can escape via two different routes. The
allosteric modulator LY2119620 turns out to hamper both
escapes routes, thus slowing down the unbinding process, as
experimentally observed. This computationally affordable
protocol is totally general, and it can be easily applied to
determine the full free energy landscape of membrane
receptors/drug interactions.},
cin = {IAS-5 / INM-9},
ddc = {610},
cid = {I:(DE-Juel1)IAS-5-20120330 / I:(DE-Juel1)INM-9-20140121},
pnm = {574 - Theory, modelling and simulation (POF3-574)},
pid = {G:(DE-HGF)POF3-574},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:30913388},
UT = {WOS:000468242900050},
doi = {10.1021/acs.jctc.9b00118},
url = {https://juser.fz-juelich.de/record/866015},
}