% IMPORTANT: The following is UTF-8 encoded. This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.
@ARTICLE{Bonus:874892,
author = {Bonus, Michele and Sommerfeld, Annika and Qvartskhava,
Natalia and Görg, Boris and Ludwig, Beatrice Stefanie and
Kessler, Horst and Gohlke, Holger and Häussinger, Dieter},
title = {{E}vidence for functional selectivity in {TUDC}- and
nor{UDCA}-induced signal transduction via α5β1 integrin
towards choleresis},
journal = {Scientific reports},
volume = {10},
number = {1},
issn = {2045-2322},
address = {[London]},
publisher = {Macmillan Publishers Limited, part of Springer Nature},
reportid = {FZJ-2020-01684},
pages = {5795},
year = {2020},
abstract = {Functional selectivity is the ligand-specific activation of
certain signal transduction pathways at a receptor and has
been described for G protein-coupled receptors. However, it
has not yet been described for ligands interacting with
integrins without αI domain. Here, we show by molecular
dynamics simulations that four side chain-modified
derivatives of tauroursodeoxycholic acid (TUDC), an agonist
of α5β1 integrin, differentially shift the conformational
equilibrium of α5β1 integrin towards the active state, in
line with the extent of β1 integrin activation from
immunostaining. Unlike TUDC, 24-nor-ursodeoxycholic acid
(norUDCA)-induced β1 integrin activation triggered only
transient activation of extracellular signal-regulated
kinases and p38 mitogen-activated protein kinase and,
consequently, only transient insertion of the bile acid
transporter Bsep into the canalicular membrane, and did not
involve activation of epidermal growth factor receptor.
These results provide evidence that TUDC and norUDCA exert a
functional selectivity at α5β1 integrin and may provide a
rationale for differential therapeutic use of UDCA and
norUDCA.},
cin = {NIC / JSC / IBI-7},
ddc = {600},
cid = {I:(DE-Juel1)NIC-20090406 / I:(DE-Juel1)JSC-20090406 /
I:(DE-Juel1)IBI-7-20200312},
pnm = {511 - Computational Science and Mathematical Methods
(POF3-511) / Forschergruppe Gohlke $(hkf7_20170501)$},
pid = {G:(DE-HGF)POF3-511 / $G:(DE-Juel1)hkf7_20170501$},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:32242141},
UT = {WOS:000540497600002},
doi = {10.1038/s41598-020-62326-y},
url = {https://juser.fz-juelich.de/record/874892},
}