ligases

Why Ligases as a Therapeutic Target?

• Ligases, similar to kinases, are a large, diverse target class with significant opportunities


• While the kinase field has matured, the ligase field is relatively novel


• Increased specificity results in reduced toxicities due to more control over the degradation of specific substrates


• Rigel and collaborators have shown that Ligase targets are a druggable target class


• The success of the proteasome inhibitor (Velcade) in the clinic, validates the therapeutic potential of the ubiquitin/proteasome system

Rigel’s Rich Ubiquitin Drug Discovery Program
Rigel is a leader in investigating and characterizing the ubiquitin ligase system for the discovery and development of potential new therapeutics. The company has initiated one of the industry's broadest efforts in working on the development of numerous ligase targets in oncology, inflammation, virology and metabolism. Rigel was one of the first companies to discover potent and highly selective small molecule inhibitors of ubiquitin ligases. Rigel has a broad-based platform in the enzymology and biology of ubiquitin ligases which includes a large number of biochemical and cell-based assays to identify the specificity and selectivity of ligase targets. This infrastructure has been established through collaborations with Merck and Daiichi. Rigel has an extensive patent portfolio covering the ligase area.


Ligase Collaboration

Daiichi-Sankyo
• Ubiquitin ligase target selected by Daiichi-Sankyo
• Rigel established/conducted HTS and 1° and 2° cell and biochemical ligase related assays
• Selective Ligase inhibitor compounds now at lead stage