Ubiquitin choke point

How Takeda’s TAK-243 safely inhibits a ubiquitination choke point in cancer

Takeda has shown its first-in-class UBA1 inhibitor could safely treat cancer by blocking a protein on which virtually all cells depend for ubiquitin-mediated protein degradation, upending conventional wisdom about how to disrupt the pathway that has focused drug developers on targets further downstream.

Three families of enzymes regulate the ubiquitination process that marks

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