The novel mechanism of lenalidomide activity - PMC
Lenalidomide acts by a novel drug mechanism—modulation of the substrate specificity of the CRL4 CRBN E3 ubiquitin ligase. In multiple myeloma, lenalidomide induces the ubiquitination …
Molecular mechanisms of thalidomide and its derivatives - PMC
Although the molecular mechanisms of thalidomide and its derivatives remained poorly understood until recently, we identified cereblon (CRBN), a primary direct target of …
The novel mechanism of lenalidomide activity
2015年11月19日 · Lenalidomide acts by a novel drug mechanism—modulation of the substrate specificity of the CRL4 CRBN E3 ubiquitin ligase. In multiple myeloma, lenalidomide induces …
Cereblon is a direct protein target for immunomodulatory and ...
The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide. Our studies demonstrate that thalidomide, lenalidomide and …
Molecular mechanism of action of immune-modulatory drugs …
A landmark study recently identified cereblon (CRBN) as a primary target of thalidomide teratogenicity. Subsequently it was demonstrated that CRBN is also required for the anti …
Discovery of CRBN as a target of thalidomide: a breakthrough for ...
2022年7月7日 · Thalidomide and its derivatives are the only protein degraders currently used in clinical practice. Our understanding of the molecular mechanism of action of thalidomide and …
The E3 ligase adapter cereblon targets the C-terminal cyclic
2022年10月19日 · The ubiquitin E3 ligase substrate adapter cereblon (CRBN) is a target of thalidomide and lenalidomide1, therapeutic agents used in the treatment of haematopoietic …
Nonclinical teratogenicity safety assessment of CRBN-engaging …
The history and magnitude of thalidomide teratogenicity and evolving understanding of the mechanisms of action (MOA) for CRBN-engaging TPDs produces a complex challenge for …
Molecular mechanisms of thalidomide and its derivatives
Although the molecular mechanisms of thalidomide and its derivatives remained poorly understood until recently, we identified cereblon (CRBN), a primary direct target of …
Structure–Activity Relationship of Potent, Selective, and Orally ...
2024年9月12日 · The original molecular glue degraders (thalidomide, lenalidomide, and pomalidomide) are known to bind to cereblon (CRBN) and alter its surface to induce …
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