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Target intelligence / Profile preview
Cereblon (CRBN)
- Target
- CRBN
- Molecular classification
- E3 ubiquitin ligase component, Substrate receptor
01
Overview
Cereblon (CRBN) is a protein that serves as a substrate receptor for the Cullin-RING E3 ubiquitin ligase complex (CRL4^CRBN), which targets specific proteins for ubiquitination and subsequent degradation. It plays a role in developmental processes, ion channel regulation, and is a key target for immunomodulatory drugs like thalidomide and its analogs. CRBN is also exploited in PROTAC technology to selectively degrade disease-relevant proteins.
- Other names
- MRT2MRT2ACereblon
02
Mechanism of action
Thalidomide and its analogs bind to cereblon, acting as "molecular glue degraders" to promote interaction between cereblon and neosubstrates, leading to their ubiquitination and proteasomal degradation.
03
Biological functions
UbiquitinationProteasomal degradationRegulation of fibroblast growth factorsIon channel regulationLimb outgrowth during embryonic developmentPresynaptic glutamate release
04
Disease associations
Intellectual disabilityCancerHematological malignancies
05
Safety considerations
Teratogenicity (Thalidomide exposure during pregnancy)Potential for off-target effects with PROTACs
06
Interacting drugs
Thalidomide
2 more in the full profile.
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