The Sound of Evolution
Thalidomide
Mechanism of action:
Thalidomide is an immunomodulatory agent. Thalidomide binds to the CRBN protein (cereblon), altering the substrate selectivity of the CRL4(CRBN) ubiquitin ligase complex and affecting the stability of specific transcription factors and regulatory proteins. Through these effects, it suppresses the production of pro-inflammatory cytokines such as TNF-α and also enhances the production of IL-2, IFN-γ, and others.
Reference(s):
1. Eriksson T et al. (2001). Clinical pharmacology of thalidomide. Eur J Clin Pharmacol.
2. Kronke J et al. (2014). Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells. Science.
3. Lepper ER et al. (2006). Thalidomide metabolism and hydrolysis: mechanisms and implications. Curr Drug Metab.