Molecular mechanisms of thalidomide and its derivatives

• Published in: Proceedings of the Japan Academy, Series B Vol. 96; no. 6; pp. 189 - 203
• Main Authors: ITO, Takumi, HANDA, Hiroshi
• Format: Journal Article
• Language: English
• Published: Japan The Japan Academy 11.06.2020
• Subjects: Animals; Beads; Blood cancer; cereblon; Chimeras; Cullin; Deoxyribonucleic acid; Derivatives; DNA; DNA repair; Drug Repositioning; Drugs; Enzymes; Erythema; FDA approval; Hematological diseases; Humans; immunomodulatory imide drugs (IMiDs); Immunotherapy; lenalidomide; Ligands; Lymphoma; Molecular modelling; Molecular Targeted Therapy; Multiple myeloma; Pharmaceutical industry; Proteins; Proteolysis; proteolysis targeting chimeras (PROTACs); Researchers; Review; Substrates; Teratogenicity; Thalidomide; Thalidomide - adverse effects; Thalidomide - chemistry; Thalidomide - pharmacology; Ubiquitin; Ubiquitin-protein ligase; United States > US; Japan; immunomodulatory imide drugs (IMiDs); cereblon; lenalidomide; thalidomide; ubiquitin; proteolysis targeting chimeras (PROTACs)

Thalidomide, originally developed as a sedative drug, causes multiple defects due to severe teratogenicity, but it has been re-purposed for treating multiple myeloma, and derivatives such as lenalidomide and pomalidomide have been developed for treating blood cancers. Although the molecular mechanis...