Target General Infomation
Target ID
T27861 (Former ID: TTDI01546)
Target Name
Protein cereblon (CRBN)
Synonyms
Protein cereblon
Gene Name
CRBN
Target Type
Clinical trial target
[1]
Disease [+] 9 Target-related Diseases +
1 Lupus erythematosus [ICD-11: 4A40]
2 Sarcoidosis [ICD-11: 4B20]
3 Brain cancer [ICD-11: 2A00]
4 Diffuse large B-cell lymphoma [ICD-11: 2A81]
5 Liver cancer [ICD-11: 2C12]
6 Lymphoma [ICD-11: 2A80-2A86]
7 Mature B-cell leukaemia [ICD-11: 2A82]
8 Multiple myeloma [ICD-11: 2A83]
9 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Function
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.
UniProt ID
CRBN_HUMAN
Sequence
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYL
GADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTF
AVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQA
KVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSW
PRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLK
IGSAIQRLRCELDIMNKCTSLCCKQCQETEITTKNEIFSLSLCGPMAAYVNPHGYVHETL
TVYKACNLNLIGRPSTEHSWFPGYAWTVAQCKICASHIGWKFTATKKDMSPQKFWGLTRS
ALLPTIPDTEDEISPDKVILCL
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 2 Clinical Trial Drugs +
1 CC-220 Drug Info Phase 2 Sarcoidosis [2]
2 CC-122 Drug Info Phase 1 Solid tumour/cancer [3]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 1 Inhibitor drugs +
1 CC-220 Drug Info [4]
Modulator [+] 1 Modulator drugs +
1 CC-122 Drug Info [1], [5]
References
REF 1 CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL. Blood. 2015 Aug 6;126(6):779-89.
REF 2 ClinicalTrials.gov (NCT02185040) A Pilot Study of CC-220 to Treat Systemic Lupus Erythematosus.. U.S. National Institutes of Health.
REF 3 ClinicalTrials.gov (NCT01421524) Study of CC-122 to Evaluate the Safety, Tolerability, and Effectiveness for Patients With Advanced Solid Tumors, Non-Hodgkin's Lymphoma, or Multiple Myeloma. U.S. National Institutes of Health.
REF 4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

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