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@ARTICLE{Lelle:874893,
author = {Lelle, Marco and Otte, Maik and Bonus, Michele and Gohlke,
Holger and Benndorf, Klaus},
title = {{F}luorophore-labeled cyclic nucleotides as potent agonists
of cyclic nucleotide-regulated ion channels},
journal = {ChemBioChem},
volume = {21},
number = {16},
issn = {1439-4227},
address = {Weinheim},
publisher = {Wiley-VCH},
reportid = {FZJ-2020-01685},
pages = {2311-2320},
year = {2020},
abstract = {High‐affinity fluorescent derivatives of cyclic adenosine
and guanosine monophosphate are powerful tools to
investigate their natural targets. Cyclic
nucleotide‐regulated ion channels belong to these targets
and are vital for many signal transduction processes, such
as vision and olfaction. The relation of ligand binding to
activation gating is still challenging and there is a
request for fluorescent probes that enable a breaking down
to the single molecule level. This inspired us to prepare
fluorophore‐labeled cyclic nucleotides, which are composed
of a bright dye and a nucleotide derivative with a
thiophenol motif at position 8 that has already been shown
to enable superior binding affinity. The preparation of
these bioconjugates was accomplished via a novel
cross‐linking strategy that involves the substitution of
the nucleobase with a modified thiophenolate in good yield.
Both fluorescent nucleotides are potent activators of
different cyclic nucleotide‐regulated ion channels with
respect to the natural ligand and previously reported
substances. Molecular docking of the probes excluding the
fluorophore reveals that the high potency can be attributed
to additional hydrophobic and cation‐π interactions
between the ligand and the protein. Moreover, the introduced
substances bear the potential to investigate related target
proteins, such as cAMP‐ and cGMP‐dependent protein
kinases, exchange proteins directly activated by cAMP or
phosphodiesterases.},
cin = {NIC / JSC / IBI-7},
ddc = {540},
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:32227403},
UT = {WOS:000530432400001},
doi = {10.1002/cbic.202000116},
url = {https://juser.fz-juelich.de/record/874893},
}