@article{oai:repo.qst.go.jp:00082791,
 author = {Honoka, Obata and Atsushi, Tsuji and Hitomi, Sudo and Aya, Sugyo and Katsuyuki, Minegishi and Kotaro, Nagatsu and Mikako, Ogawa and Zhang, Ming-Rong and Honoka, Obata and Atsushi, Tsuji and Hitomi, Sudo and Aya, Sugyo and Katsuyuki, Minegishi and Kotaro, Nagatsu and Mikako, Ogawa and Zhang, Ming-Rong},
 issue = {9},
 journal = {International Journal of Molecular Sciences},
 month = {May},
 note = {Due to their short-range (2–500 nm), Auger electrons (Auger e????) have the potential to
induce nano-scale physiochemical damage to biomolecules. Although DNA is the primary target of
Auger e????, it remains challenging to maximize the interaction between Auger e???? and DNA. To assess
the DNA-damaging effect of Auger e???? released as close as possible to DNA without chemical damage,
we radio-synthesized no-carrier-added (n.c.a.) [189, 191Pt]cisplatin and evaluated both its in vitro
properties and DNA-damaging effect. Cellular uptake, intracellular distribution, and DNA binding
were investigated, and DNA double-strand breaks (DSBs) were evaluated by immunofluorescence
staining of 
H2AX and gel electrophoresis of plasmid DNA. Approximately 20% of intracellular radio-
Pt was in a nucleus, and about 2% of intra-nucleus radio-Pt bound to DNA, although uptake of n.c.a.
radio-cisplatin was low (0.6% incubated dose after 25-h incubation), resulting in the frequency of cells
with 
H2AX foci was low (1%). Nevertheless, some cells treated with radio-cisplatin had 
H2AX
aggregates unlike non-radioactive cisplatin. These findings suggest n.c.a. radio-cisplatin binding to
DNA causes severe DSBs by the release of Auger e???? very close to DNA without chemical damage
by carriers. Efficient radio-drug delivery to DNA is necessary for successful clinical application of
Auger e????.
Keywords: Auger electron; cisplatin; 191Pt; 189Pt; radio-drug; DNA double-strand break; 
H2AX},
 title = {In Vitro Evaluation of No-Carrier-Added Radiolabeled Cisplatin ([189, 191Pt]cisplatin) Emitting Auger Electrons},
 volume = {22},
 year = {2021}
}