New mechanism of lenalidomide activity

Jacob Keevan, William D. Figg*

*Corresponding author for this work

Research output: Contribution to journalComment/debate

1 Scopus citations


Lenalidomide is an immunomodulatory agent (IMiD) that has activity in hematologic cancer (e.g., multiple myeloma). The immunomodulatory and apoptotic properties are readily apparent in therapy. However, the exact mechanism of action has been difficult to quantify until recently when it was shown that another IMiD, thalidomide, binds to an E3 ubiquitin ligase complex constituent, CRBN.1 The article by Kronke et al. demonstrates that, by binding to CRBN and altering its selectivity, lenalidomide potentiates the ubiquitination and proteolysis of 2 specific proteins, IKZF1 and IKZF3. An article in the same issue, by Lu et al., supports these observations.2,3 IKZF1 and IKZF3 are transcription factors that are necessary for multiple myeloma, and repression of these transcription factors is a likely mechanism for lenalidomide activity in this disease.

Original languageEnglish
Pages (from-to)968-969
Number of pages2
JournalCancer Biology and Therapy
Issue number8
StatePublished - Aug 2014
Externally publishedYes


  • CRBN
  • IKZF1
  • IKZF1/3
  • IKZF3
  • IMiD
  • Immunomodulatory agent
  • Lenalidomide


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