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Target intelligence / Profile preview
E3 Ubiquitin-Protein Ligase Cereblon (CRBN)
- Target
- CRBN
- Molecular classification
- E3 ubiquitin ligase, Substrate receptor, RING-type multi-subunit E3 ligase
01
Overview
Cereblon (CRBN) is a substrate receptor within the Cullin-RING E3 ubiquitin ligase complex CRL4^CRBN. It confers substrate specificity, recognizing and binding target proteins, facilitating their polyubiquitination and subsequent proteasomal degradation. Its interaction with immunomodulatory drugs (IMiDs) like thalidomide is central to their pharmacological effects, but also leads to teratogenicity. Mutations are associated with intellectual disability.
- Other names
- MRT2MRT2ACereblon
02
Mechanism of action
IMiDs bind cereblon, altering its substrate specificity and leading to ubiquitination and proteasome-mediated degradation of neo-substrates.
03
Biological functions
UbiquitinationProteasomal targetingDevelopmental regulationNeuronal functionCellular metabolismSignal transduction
04
Disease associations
Intellectual disabilityMultiple myelomaCancerNeurodevelopmental disorders
05
Safety considerations
TeratogenicityOff-target protein degradation
06
Interacting drugs
Thalidomide
2 more in the full profile.
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