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@ARTICLE{Otte:863298,
author = {Otte, Maik and Schweinitz, Andrea and Lelle, Marco and
Thon, Susanne and Enke, Uta and Yüksel, Sezin and
Schmauder, Ralf and Bonus, Michele and Gohlke, Holger and
Benndorf, Klaus},
title = {{N}ovel {F}luorescent {C}yclic {N}ucleotide {D}erivatives
to {S}tudy {CNG} and {HCN} {C}hannel {F}unction},
journal = {Biophysical journal},
volume = {116},
number = {12},
issn = {0006-3495},
address = {Bethesda, Md.},
publisher = {Soc.},
reportid = {FZJ-2019-03385},
pages = {2411-2422},
year = {2019},
abstract = {A highly specific molecular interaction of diffusible
ligands with their receptors belongs to the key processes in
cellular signaling. Because an appropriate method to monitor
the unitary binding events is still missing, most of our
present knowledge is based on ensemble signals recorded from
a big number of receptors, such as ion currents or
fluorescence changes of suitably labeled receptors, and
reasoning from these data to the ligand binding. To study
the binding process itself, appropriately tagged ligands are
required that fully activate the receptors and report the
binding at the same time. Herein, we tailored a series of 18
novel fluorescent cyclic nucleotide derivatives by attaching
6 different dyes via different alkyl linkers to the
8-position of the purine ring of cGMP or cAMP. The
biological activity was determined in inside-out
macropatches containing either homotetrameric (CNGA2),
heterotetrameric (CNGA2:CNGA4:CNGB1b), or
hyperpolarization-activated cyclic nucleotide-modulated
(HCN2) channels. All these novel fluorescent ligands are
efficient to activate the channels, and the potency of most
of them significantly exceeded that of the natural cyclic
nucleotides cGMP or cAMP. Moreover, some of them showed an
enhanced brightness when bound to the channels. The best of
our derivatives bear great potential to systematically
analyze the activation mechanism in CNG and HCN channels, at
both the level of ensemble and single-molecule analyses.},
cin = {JSC / NIC / ICS-6},
ddc = {570},
cid = {I:(DE-Juel1)JSC-20090406 / I:(DE-Juel1)NIC-20090406 /
I:(DE-Juel1)ICS-6-20110106},
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:31130235},
UT = {WOS:000471862300019},
doi = {10.1016/j.bpj.2019.05.006},
url = {https://juser.fz-juelich.de/record/863298},
}