| Literature DB >> 26512454 |
Andrew A Guirguis1, Benjamin L Ebert2.
Abstract
Lenalidomide and its related 'analogues' modulate the substrate specificity of the CRL4(CRBN) E3 ubiquitin ligase complex. Polyubiquitination and subsequent proteasomal degradation of IKZF1 and IKZF3 in multiple myeloma and CK1α in del(5q) MDS has recently been linked to therapeutic efficacy of this class of compounds. Harnessing ubiquitin ligase substrate specificity, may in time facilitate the degradation of other 'undruggable' proteins and allow for separation of detrimental side effects of IMiD compounds from those associated with therapeutic efficacy.Entities:
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Year: 2015 PMID: 26512454 DOI: 10.1016/j.ceb.2015.10.004
Source DB: PubMed Journal: Curr Opin Cell Biol ISSN: 0955-0674 Impact factor: 8.382