Selective Targeting of the KRAS Codon12 Mutation Sequence by Pyrrole-Imidazole Polyamide seco-CBI Conjugates

• Published in: Chemistry : a European journal Vol. 21; no. 42; pp. 14996 - 15003
• Main Authors: Taylor, Rhys D, Chandran, Anandhakumar, Kashiwazaki, Gengo, Hashiya, Kaori, Bando, Toshikazu, Nagase, Hiroki, Sugiyama, Hiroshi
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley Subscription Services, Inc 12.10.2015
• Subjects: Affinity; Alkylation; Cancer; Chemistry; Conjugates; Mutation; Mutations; Optimization; Polyamide resins; Sequencing

Mutation of KRAS is a key step in many cancers. Mutations occur most frequently at codon12, but the targeting of KRAS is notoriously difficult. We recently demonstrated selective reduction in the volume of tumors harboring the KRAS codon12 mutation in a mouse model by using an alkylating hairpin N-m...