Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs

Sophie Day-Riley1, Sona Krajcovicova1,2, Aryaman Raj Sokhal1

  • 1Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, United Kingdom.

Insights

Researchers developed novel PROTACs to degrade human protein kinase CK2, a cancer target. These PROTACs offer potential for more effective and selective cancer therapy than traditional inhibitors.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Human protein kinase CK2 (CK2) is a serine/threonine kinase constitutively active in numerous cancers.
  • Current ATP-competitive inhibitors like CX-4945 have limitations including off-target effects and incomplete CK2 suppression.

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