2020年11月17日
DNA Alkylation of the RUNX-Binding Sequence by CBI-PI Polyamide Conjugates*.
Chemistry (Weinheim an der Bergstrasse, Germany)
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- 巻
- 26
- 号
- 64
- 開始ページ
- 14639
- 終了ページ
- 14644
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1002/chem.202002166
Many types of molecular targeted drugs that inhibit cancer growth by acting on specific molecules have been developed. The runt-related transcription factor (RUNX) family, which induces cancer development by binding to a specific DNA sequence, has attracted attention as a new target for cancer treatment. We have developed Chb-M', which targets the RUNX-binding sequence. Chb-M' was developed by conjugating pyrrole-imidazole (PI) polyamides and chlorambucil as an anticancer agent. It was recently reported that Chb-M' had a remarkable anticancer effect in vivo. In this study, to explore the possibility of an alternative structure, we designed a new series of CBI-PI polyamides, in which seco-CBI was applied as a DNA-alkylating agent. We examined the characteristics of the CBI-PI polyamides targeting the RUNX-binding sequence and found that these conjugates have great potential for cancer treatment.
- ID情報
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- DOI : 10.1002/chem.202002166
- PubMed ID : 32672369