DNA damage repair plays key roles not only in maintaining genome integrity but also in reducing the antitumor efficacy of DNA-damaging antineoplastics. In their Communication on
page 15564 ff., G.
Zhu et al. describe a Pt
IV anticancer prodrug targeting nucleotide excision repair (NER) to overcome cisplatin resistance. This dual-action prodrug with both cisplatin and NER inhibitor moieties causes DNA damage and inhibits NER, which leads to significantly increased cytotoxicity in cisplatin-resistant human cancer cells.