Article
The cryo-EM structure of the SF3b spliceosome complex bound to a splicing modulator reveals a pre-mRNA substrate competitive mechanism of action.
Genes & development - 1 Feb 2018
Finci Lorenzo I, Zhang Xiaofeng, Huang Xiuliang, Zhou Qiang, Tsai Jennifer, Teng Teng, Agrawal Anant, Chan Betty, Irwin Sean, Karr Craig, Cook Andrew, Zhu Ping, Reynolds Dominic, Smith Peter G, Fekkes Peter, Buonamici Silvia, Larsen Nicholas A
Abstract excerpt
Somatic mutations in spliceosome proteins lead to dysregulated RNA splicing and are observed in a variety of cancers. These genetic aberrations may offer a potential intervention point for targeted therapeutics. SF3B1, part of the U2 small nuclear RNP (snRNP), is targeted by splicing modulators, including E7107, the first to enter clinical trials, and, more recently, H3B-8800. Modulating splicing represents a...
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