Tclin CRBN Protein cereblon

Protein Summary

Description

Substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins, such as MEIS2. Normal degradation of key regulatory proteins is required for normal limb outgrowth and expression of the fibroblast growth factor FGF8. May play a role in memory and learning by regulating the assembly and neuronal surface expression of large-conductance calcium-activated potassium channels in brain regions involved in memory and learning via its interaction with KCNT1. Binding of pomalidomide and other thalidomide-related drugs changes the substrate specificity of the human protein, leading to decreased degradation of MEIS2 and other target proteins and increased degradation of MYC, IRF4, IKZF1 and IKZF3. This gene encodes a protein related to the Lon protease protein family. In rodents and other mammals this gene product is found in the cytoplasm localized with a calcium channel membrane protein, and is thought to play a role in brain development. Mutations in this gene are associated with autosomal recessive nonsyndromic cognitive disability. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Mar 2010]

Uniprot Accession IDs

• Q96SW2
• B2R6H4
• C9IZA9
• C9JAH6
• Q6AI62
• Q6NVZ0
• Q9UHW4

Gene Name

• CRBN

Ensembl ID

• ENST00000231948
• ENSP00000231948
• ENSG00000113851
• ENST00000432408
• ENSP00000412499

Symbol

• MRT2
• MRT2A

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
kinase perturbation	0.98
transcription factor perturbation	0.97
protein complex	0.93
transcription factor binding site profile	0.73
cellular component	0.72

Protein Classes

PANTHER Classes

Protein / Hydrolase / Protein Cereblon

DTO Classes

Protein / Enzyme / Hydrolase / Protein Cereblon

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 403.34   (req: < 5)

Gene RIFs: 80   (req: <= 3)

Antibodies: 123   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 403.34   (req: >= 5)

Gene RIFs: 80   (req: > 3)

Antibodies: 123   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 6

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 9

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 3