DNA Alkylation of the RUNX‐Binding Sequence by CBI–PI Polyamide Conjugates**
| Autor: | Rina Maeda, Kaori Hashiya, Toshikazu Bando, Hiroshi Sugiyama, Shinji Ito |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Alkylation
010405 organic chemistry Drug discovery Chemistry Organic Chemistry Imidazoles Cancer Sequence (biology) DNA General Chemistry 010402 general chemistry medicine.disease 01 natural sciences Catalysis DNA sequencing 0104 chemical sciences Nylons DNA Alkylation Biochemistry In vivo Drug delivery medicine Pyrroles Transcription factor |
| Zdroj: | Chemistry – A European Journal. 26:14639-14644 |
| ISSN: | 1521-3765 0947-6539 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
| Nepřihlášeným uživatelům se plný text nezobrazuje | K zobrazení výsledku je třeba se přihlásit. |