Skip to content
2000
Volume 18, Issue 19
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X

Abstract

Casein kinase 2 (CK2) is a ubiquitous, highly pleiotropic and essential protein kinase whose abnormally high constitutive activity has been implicated in several human diseases. In the last decade, several ATP competitive inhibitors of CK2, characterized by an in vitro activity that ranges from micromolar to nanomolar, have been discovered. However, until now only one drug candidate has been entered in Phase I clinical trial as a potential anticancer drug. Why this constitutively active kinase is so undruggable? Can ATP competitive inhibitors be considered the most promising drug candidates for the near future? In this review, we would like to underline how targeting binding sites outside the conventional ATP-binding could represent a new promising strategy to inhibit CK2 activity and, consequently, bear a great potentiality in discovering new drug candidates.

Loading

Article metrics loading...

/content/journals/cmc/10.2174/092986711796150423
2011-06-01
2025-05-05
Loading full text...

Full text loading...

/content/journals/cmc/10.2174/092986711796150423
Loading

  • Article Type:
    Research Article
Keyword(s): CK2 in human diseases; Kinase Inhibitors; Protein kinase CK2
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test