Article
Identification of Binding Targets of a Pyrrole-Imidazole Polyamide KR12 in the LS180 Colorectal Cancer Genome.
PloS one - 1 Jan 2016
Lin Jason, Hiraoka Kiriko, Watanabe Takayoshi, Kuo Tony, Shinozaki Yoshinao, Takatori Atsushi, Koshikawa Nobuko, Chandran Anandhakumar, Otsuki Joe, Sugiyama Hiroshi, Horton Paul, Nagase Hiroki
Abstract excerpt
Pyrrole-imidazole polyamides are versatile DNA minor groove binders and attractive therapeutic options against oncological targets, especially upon functionalization with an alkylating agent such as seco-CBI. These molecules also provide an alternative for oncogenes deemed "undruggable" at the protein level, where the absence of solvent-accessible pockets or structural crevices prevent the formation of...
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