Protein kinase CK2 inhibition as a pharmacological strategy

Adv Protein Chem Struct Biol. 2021:124:23-46. doi: 10.1016/bs.apcsb.2020.09.003. Epub 2021 Jan 9.

Abstract

CK2 is a constitutively active Ser/Thr protein kinase which phosphorylates hundreds of substrates. Since they are primarily related to survival and proliferation pathways, the best-known pathological roles of CK2 are in cancer, where its targeting is currently being considered as a possible therapy. However, CK2 activity has been found instrumental in many other human pathologies, and its inhibition will expectably be extended to different purposes in the near future. Here, after a description of CK2 features and implications in diseases, we analyze the different inhibitors and strategies available to target CK2, and update the results so far obtained by their in vivo application.

Keywords: CK-II; CK2; CX-4945; Cancer; Casein kinase 2; Kinase inhibitors; Silmitasertib.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Casein Kinase II* / antagonists & inhibitors
  • Casein Kinase II* / metabolism
  • Drug Delivery Systems*
  • Humans
  • Neoplasm Proteins* / antagonists & inhibitors
  • Neoplasm Proteins* / metabolism
  • Neoplasms* / drug therapy
  • Neoplasms* / enzymology
  • Protein Kinase Inhibitors / therapeutic use*

Substances

  • Neoplasm Proteins
  • Protein Kinase Inhibitors
  • Casein Kinase II