Nek2 proteolysis targeting chimeras for use in malignant disease

This invention describes a small molecule proteolysis targeting chimera (PROTAC) strategy to degrade the NEK2 (Never in Mitosis Related Kinase 2) protein and methods of use thereof. The NEK2 PROTAC consists of three, key regions: a NEK2 ligand to bind the NEK2 protein, a linker region to link the NEK2 ligand to a ligase ligand, and the ligase ligand.

ABSTRACT

This invention describes a small molecule proteolysis targeting chimera (PROTAC) strategy to degrade the NEK2 (Never in Mitosis Related Kinase 2) protein and methods of use thereof. The NEK2 PROTAC consists of three, key regions: a NEK2 ligand to bind the NEK2 protein, a linker region to link the NEK2 ligand to a ligase ligand, and the ligase ligand.

CLAIMS

1 A proteolysis targeting chimera of formula LL-L-NBL, wherein NBL is a EK2 binding ligand, LL is a ligase ligand, and L is a linker-region to link the NEK2 ligand to the ligase ligand.

PATENT INFORMATION


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