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Target intelligence / Profile preview
CRL4CRBN E3 Ligase Complex (CRL4CRBN)
- Target
- CRL4CRBN
- Molecular classification
- E3 ubiquitin ligase complex, Multi-protein complex, Enzyme
01
Overview
The CRL4CRBN E3 ligase complex is a multi-protein ubiquitin ligase that mediates targeted protein degradation via the ubiquitin-proteasome system. It comprises CUL4, DDB1, ROC1/RBX1, and CRBN. CRBN acts as a substrate receptor, and its interaction with drugs like IMiDs alters substrate specificity, leading to the degradation of neosubstrates. This complex is a key therapeutic target, especially in multiple myeloma, and is exploited by PROTACs for targeted protein degradation.
- Other names
- Cereblon E3 ligase complexCUL4-DDB1-ROC1-CRBN complex
02
Mechanism of action
The CRL4CRBN E3 ligase complex mediates the transfer of ubiquitin from an E2 enzyme to specific substrate proteins, marking them for proteasomal degradation. IMiDs bind to CRBN, altering its substrate specificity and leading to the degradation of neosubstrates. PROTACs recruit target proteins for ubiquitination and degradation.
03
Biological functions
UbiquitinationProtein degradationCell cycle regulationProtein homeostasisSubstrate receptor activity
04
Disease associations
CancerMultiple myelomaHematological malignancies
05
Safety considerations
Teratogenicity (Thalidomide)Drug resistanceOff-target effects of PROTACsMyelosuppression
06
Interacting drugs
Thalidomide
6 more in the full profile.
07
Biomarkers
CRBN expression levelsCUL4B mutationsDDB1 mutationsIKZF1/IKZF3 levels
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