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The Evolving Tale of Immunomodulatory Drugs and Cereblon
Author(s) -
Holstein S A
Publication year - 2014
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.2014.168
Subject(s) - cereblon , thalidomide , clinical pharmacology , ubiquitin ligase , molecular pharmacology , pharmacology , multiple myeloma , mechanism of action , ubiquitin , computational biology , medicine , chemistry , biology , immunology , biochemistry , gene , receptor , in vitro
The immunomodulatory drugs (IMiDs), of which thalidomide was the first in class, have had a complex therapeutic history. Although these drugs are now widely used to treat multiple myeloma, the precise molecular mechanism of action of these agents has remained elusive. The finding that IMiDs bind cereblon, with subsequent activation of E3‐ubiquitin ligase activity and degradation of the key transcription factors IKZF1 and IKZF3, has provided insight into these drugs but leaves many questions unanswered. Clinical Pharmacology & Therapeutics (2014); 96 5, 538–541. doi: 10.1038/clpt.2014.168