CREB binding protein

Target id: 2734

Nomenclature: CREB binding protein

Family: Non-enzymatic BRD containing proteins

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     CREB binding protein has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2442 16p13.3 CREBBP CREB binding protein
Mouse - 2441 16 A1 Crebbp CREB binding protein
Rat - 2444 10q12 Crebbp CREB binding protein
Previous and Unofficial Names
RSTS | Rubinstein-Taybi syndrome
Database Links
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution NMR structure of ischemin bound to the bromodomain of CBP.
PDB Id:  2L84
Ligand:  ischemin
Resolution:  0.0Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Solution NMR structure showing the association of MS7072 with the bromodomain of CBP.
PDB Id:  2D82
Ligand:  MS7972
Resolution:  0.0Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the bromodomain of human CREBBP in complex with SGC-CBP30
PDB Id:  4NR7
Ligand:  SGC-CBP30
Resolution:  1.2Å
Species:  Human
References: 

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
I-CBP112 Hs Inhibition 6.8 pKd 5
pKd 6.8 (Kd 1.42x10-7 M) [5]
Description: Isothermal titration calorimetry (ITC) assay.
ischemin Hs Inhibition 4.7 pKd 1
pKd 4.7 (Kd 1.9x10-5 M) [1]
Description: Binding to CBP's bromodomain (amino acid residues 1081-1197)
SGC-CBP30 Hs Inhibition 7.2 pIC50 3
pIC50 7.2 (IC50 6.9x10-8 M) [3]
compound 50 [PMID: 24313754] Hs Inhibition 6.2 pIC50 2
pIC50 6.2 (IC50 6.31x10-7 M) [2]
Immunopharmacology Comments
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. PMID: 26261308
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045637 regulation of myeloid cell differentiation TAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
GO:0045637 regulation of myeloid cell differentiation TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0032481 positive regulation of type I interferon production TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
Clinically-Relevant Mutations and Pathophysiology
Disease:  Acute myeloid leukemia with t(8;16)(p11;p13) translocation
Orphanet: ORPHA370026
Disease:  Chromosome 16p13.3 deletion syndrome
Synonyms: Rubinstein-Taybi syndrome due to 16p13.3 microdeletion [Orphanet: ORPHA353281]
OMIM: 610543
Orphanet: ORPHA353281
Disease:  Rubinstein-Taybi syndrome 1; RSTS1
Synonyms: Rubinstein-Taybi syndrome [Disease Ontology: DOID:1933]
Rubinstein-Taybi syndrome due to CREBBP mutations [Orphanet: ORPHA353277]
Disease Ontology: DOID:1933
OMIM: 180849
Orphanet: ORPHA353277

References

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1. Borah JC, Mujtaba S, Karakikes I, Zeng L, Muller M, Patel J, Moshkina N, Morohashi K, Zhang W, Gerona-Navarro G et al.. (2011) A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. Chem. Biol., 18 (4): 531-41. [PMID:21513889]

2. Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I et al.. (2014) [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. J. Med. Chem., 57 (2): 462-76. [PMID:24313754]

3. Gallenkamp D, Gelato KA, Haendler B, Weinmann H. (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem, 9 (3): 438-64. [PMID:24497428]

4. Sachchidanand, Resnick-Silverman L, Yan S, Mutjaba S, Liu WJ, Zeng L, Manfredi JJ, Zhou MM. (2006) Target structure-based discovery of small molecules that block human p53 and CREB binding protein association. Chem. Biol., 13 (1): 81-90. [PMID:16426974]

5. SGC. I-CBP112 - a CREBBP/EP300-selective chemical probe. Accessed on 03/03/2015. Modified on 03/03/2015. thesgc.org, http://www.thesgc.org/chemical-probes/ICBP112

How to cite this page

Non-enzymatic BRD containing proteins: CREB binding protein. Last modified on 23/03/2016. Accessed on 23/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2734.