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@ARTICLE{Suku:834631,
author = {Suku, Eda and Fierro, Fabrizio and Giorgetti, Alejandro and
Alfonso-Prieto, Mercedes and Carloni, Paolo},
title = {{M}ulti-scale simulations of membrane proteins: {T}he case
of bitter taste receptors},
journal = {Journal of science},
volume = {2},
number = {1},
issn = {2468-2179},
address = {Amsterdam},
publisher = {Elsevier},
reportid = {FZJ-2017-04539},
pages = {15 - 21},
year = {2017},
abstract = {Human bitter taste receptors (hTAS2Rs) are the second
largest group of chemosensory G-protein coupled receptors
(25 members). hTAS2Rs are expressed in many tissues (e.g.
tongue, gastrointestinal tract, respiratory system, brain,
etc.), performing a variety of functions, from bitter taste
perception to hormone secretion and bronchodilation. Due to
the lack of experimental structural information,
computations are currently the methods of choice to get
insights into ligand–receptor interactions. Here we review
our efforts at predicting the binding pose of agonists to
hTAS2Rs, using state-of-the-art bioinformatics approaches
followed by hybrid Molecular Mechanics/Coarse-Grained
(MM/CG) simulations. The latter method, developed by us,
describes atomistically only the agonist binding region,
including hydration, and it may be particularly suited to be
used when bioinformatics predictions generate very
low-resolution models, such as the case of hTAS2Rs. Our
structural predictions of the hTAS2R38 and hTAS2R46
receptors in complex with their agonists turn out to be
fully consistent with experimental mutagenesis data. In
addition, they suggest a two-binding site architecture in
hTAS2R46, consisting of the usual orthosteric site together
with a “vestibular” site toward the extracellular space,
as observed in other GPCRs. The presence of the vestibular
site may help to discriminate among the wide spectrum of
bitter ligands},
cin = {IAS-5 / INM-9},
ddc = {600},
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},
UT = {WOS:000407868100002},
doi = {10.1016/j.jsamd.2017.03.001},
url = {https://juser.fz-juelich.de/record/834631},
}