Mdm2 targeting via PROteolysis TArgeting Chimeras (PROTAC) is efficient in p53 wildtype, p53-mutated, and abemaciclib-resistant estrogen receptor-positive cell lines and superior to mdm2 inhibition.

Abstract excerpt

PURPOSE: The human double minute 2 homolog hdm2, alias mdm2, is the main negative-regulator of the tumor suppressor p53. In that capacity, mdm2 is a promising but not yet utilized molecular target for the treatment of breast cancer, however, its inhibition by small molecules is rather inappropriate. Instead, mdm2 degradation by PROteolysis TArgeting Chimeras (PROTAC) is expected to be highly specific, to exhibit...

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