DNA Alkylation of the RUNX-Binding Sequence by CBI-PI Polyamide Conjugates*.

Chemistry : a European Journal
Rina MaedaHiroshi Sugiyama

Abstract

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.

References

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Jan 3, 2019·Journal of the American Chemical Society·Rina MaedaHiroshi Sugiyama

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Citations

Jan 17, 2021·Chembiochem : a European Journal of Chemical Biology·Rina MaedaHiroshi Sugiyama

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Chembiochem : a European Journal of Chemical Biology
Rina MaedaHiroshi Sugiyama
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