title: [Thalidomide, cereblon and multiple myeloma].
abstract: Cereblon was identified as a direct target of thalidomide by Prof. H. Handa, and this pioneering work triggered active research on IMiDs (immunomodulatory drugs), which include thalidomide-derivatives, such as lenalidomide and pomalidomide. These small molecules have been shown to bind to cereblon (CRBN) to modulate its activity as a substrate receptor. In addition, structural analyses on CRBN have revealed unique actions of these small agents, by which degradation of transcription factors is controlled in a specific and unique way. I summarize recent progress on CRBN-CRLA ubiquitin ligase and IMiDs, focusing on the therapeutic application of these drugs for treatment of multiple myeloma.
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Ogura
mesh_terms: D048868:Adaptor Proteins, Signal Transducing; D006801:Humans; D051740:Ikaros Transcription Factor / Q000737:chemistry / Q000378:metabolism; D009101:Multiple Myeloma / Q000188:drug therapy* / Q000378:metabolism; D010447:Peptide Hydrolases / Q000378:metabolism*; D011485:Protein Binding; D013792:Thalidomide / Q000737:chemistry / Q000627:therapeutic use*; D044767:Ubiquitin-Protein Ligases
chemical_list: D048868:Adaptor Proteins, Signal Transducing; C502543:CRBN protein, human; C497239:IKZF1 protein, human; D051740:Ikaros Transcription Factor; D013792:Thalidomide; D044767:Ubiquitin-Protein Ligases; D010447:Peptide Hydrolases