Abstract:
:The AP sites are representative of DNA damage and known as an intermediate in the base excision repair (BER) pathway which is involved in the repair of damaged nucleobases by reactive oxygen species, UVA irradiation, and DNA alkylating agents. Therefore, it is expected that the inhibition or modulation of the AP site repair pathway may be a new type of anticancer drug. In this study, we investigated the effects of the thioguanine-polyamine ligands (SG-ligands) on the affinity and the reactivity for the AP site under UVA irradiated and non-irradiated conditions. The SG-ligands have a photo-reactivity with the A-F-C sequence where F represents a tetrahydrofuran AP site analogue. Interestingly, the SG-ligands promoted the β-elimination of the AP site followed by the formation of a covalent bond with the β-eliminated fragment without UVA irradiation.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Abe YS,Sasaki Sdoi
10.1016/j.bmc.2019.115160subject
Has Abstractpub_date
2019-12-15 00:00:00pages
115160issue
24eissn
0968-0896issn
1464-3391pii
S0968-0896(19)31280-5journal_volume
27pub_type
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