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@INPROCEEDINGS{Dahmen:841328,
author = {Dahmen, Volker and Kriehuber, Ralf},
title = {125{I}-labelled {T}riplex-forming-oligonucleotides:
{S}tudies on intracellular distribution and on gene
expression alterations of target genes},
reportid = {FZJ-2017-08413},
year = {2010},
abstract = {Purpose: Triplex-forming-oligonucleotides (TFOs) are able
to bind DNA in a sequence specific manner and are a
promising tool to manipulate genes or gene regulatory units
in a cellular environment. TFOs might have also therapeutic
potential e.g. as a carrier molecule for
Auger-Electron-Emitter (AEE) to target specific DNA
structures of tumour cells. We established a method for the
effective labelling of TFOs with the AEE 125I and studied
the DNA binding capabilities of labelled TFOs in vitro.
Furthermore the intracellular biokinetic of TFOs and the
influence of 125I-labelled TFOs on their specific target
genes in vitro were examined. Methods: TFOs specific for the
genes cdkn2a, bcl2, brca1, chk2, cdk4 were designed using
TFO Target Sequence Search (Univ. of Texas). TFO labelling
with 125I was performed using the primer extension method.
Formation of DNA triplexes was visualized with MS Imaging
Plates employing a FLA-5000 Imaging System (Fujifilm,
Düsseldorf) and electrophoretic-mobility-shift-assay
(EMSA). For biokinetic studies SCL-II cells were transfected
by electroporation (Amaxa transfector) with
Alexa488-labelled TFOs. Transfected cells were subsequently
cultured for 1, 6, 12, 18, 24, 30, 48 and 72 h and TFO
signal intensity was determined in single cells and in
isolated cell nuclei by flow cytometry (FACS-Canto II, BD).
SCL-II cells transfected with 125I-labelled TFOs were
cultured for 24 h and stored at -150 °C for decay
accumulation for at least one half-life. Alteration of gene
expression was detected with quantitative Real-Time PCR on a
7500 Real Time PCR System (Applied Biosystems, Darmstadt)
Results: The desired DNA-Triplex-formation could be
confirmed in vitro by EMSA for 52.6 $\%$ (n = 10/ 19) of all
tested TFOs and by autoradiographic analysis for 10.5 $\%$
(n = 2/ 19) of all investigated 125I-labelled TFOs. The
biokinetic studies showed that TFO-Alexa488-positive cells
were detectable as soon as 1 h after transfection. A
substantial loss of TFO-Alexa488-labelled positive cell
nuclei was observed within the first 6 h post-transfection
followed by a significant increase up to 18 h
post-transfection. The signal intensity remained constant
for at least 30 h. 72 h after transfection the TFO signal
decreased significantly but was still detectable. The
transfection of SCL-II cells with 125I-labelled TFOs lead to
a 1.7-times increased expression of the target gene when
compared to sham-transfected negative control.Conclusions:
Labelling of TFOs with 125I has a strong influence on their
DNA-Triplex-forming capacities. TFOs initially located in
the cytoplasm re-locate to the cell nucleus within 12 h
after delivery of the TFOs probably during cell division.
125I-labelled TFOs can significantly alter gene expression
in vitro.Supported by BMBF, Kompetenzverbund für
Strahlenforschung (KVSF)},
month = {Sep},
date = {2010-09-01},
organization = {13. Jahrestagung der Gesellschaft für
Biologische Strahlenforschung, Hamburg
(Germany), 1 Sep 2010 - 2 Sep 2010},
subtyp = {After Call},
cin = {S-US},
cid = {I:(DE-Juel1)S-US-20090406},
pnm = {899 - ohne Topic (POF3-899)},
pid = {G:(DE-HGF)POF3-899},
typ = {PUB:(DE-HGF)24},
url = {https://juser.fz-juelich.de/record/841328},
}