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@ARTICLE{Biarns:201341,
author = {Biarnés, Xevi and Marchiori, Alessandro and Giorgetti,
Alejandro and Lanzara, Carmela and Gasparini, Paolo and
Carloni, Paolo and Born, Stephan and Brockhoff, Anne and
Behrens, Maik and Meyerhof, Wolfgang},
title = {{I}nsights into the {B}inding of {P}henyltiocarbamide
({PTC}) {A}gonist to {I}ts {T}arget {H}uman {TAS}2{R}38
{B}itter {R}eceptor},
journal = {PLoS one},
volume = {5},
number = {8},
issn = {1932-6203},
address = {Lawrence, Kan.},
publisher = {PLoS},
reportid = {FZJ-2015-03638},
pages = {e12394 -},
year = {2010},
abstract = {Humans' bitter taste perception is mediated by the hTAS2R
subfamily of the G protein-coupled membrane receptors
(GPCRs). Structural information on these receptors is
currently limited. Here we identify residues involved in the
binding of phenylthiocarbamide (PTC) and in receptor
activation in one of the most widely studied hTAS2Rs
(hTAS2R38) by means of structural bioinformatics and
molecular docking. The predictions are validated by
site-directed mutagenesis experiments that involve specific
residues located in the putative binding site and
trans-membrane (TM) helices 6 and 7 putatively involved in
receptor activation. Based on our measurements, we suggest
that (i) residue N103 participates actively in PTC binding,
in line with previous computational studies. (ii) W99, M100
and S259 contribute to define the size and shape of the
binding cavity. (iii) W99 and M100, along with F255 and
V296, play a key role for receptor activation, providing
insights on bitter taste receptor activation not emerging
from the previously reported computational models.},
cin = {GRS / IAS-5},
ddc = {500},
cid = {I:(DE-Juel1)GRS-20100316 / I:(DE-Juel1)IAS-5-20120330},
pnm = {899 - ohne Topic (POF2-899)},
pid = {G:(DE-HGF)POF2-899},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000281234700019},
pubmed = {20811630},
doi = {10.1371/journal.pone.0012394},
url = {https://juser.fz-juelich.de/record/201341},
}