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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 | |
Alphafold | Q92793 (Hs) |
CATH/Gene3D | 1.10.1630.10, 1.20.1020.10, 1.20.920.10 |
ChEMBL Target | CHEMBL5747 (Hs) |
Ensembl Gene | ENSG00000005339 (Hs), ENSMUSG00000022521 (Mm), ENSRNOG00000005330 (Rn) |
Entrez Gene | 1387 (Hs), 12914 (Mm), 54244 (Rn) |
Human Protein Atlas | ENSG00000005339 (Hs) |
KEGG Gene | hsa:1387 (Hs), mmu:12914 (Mm), rno:54244 (Rn) |
OMIM | 600140 (Hs) |
Pharos | Q92793 (Hs) |
RefSeq Nucleotide | NM_004380 (Hs), NM_001025432 (Mm), NM_133381 (Rn) |
RefSeq Protein | NP_004371 (Hs), NP_001020603 (Mm), NP_596872 (Rn) |
SynPHARM |
79896 (in complex with ischemin) 79941 (in complex with SGC-CBP30) |
UniProtKB | Q92793 (Hs) |
Wikipedia | CREBBP (Hs) |
Selected 3D Structures | |||||||||||||
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Download all structure-activity data for this target as a CSV file
Activators | |||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Other Binding Ligands | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. PMID: 26261308 |
Immuno Process Associations | ||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||||||
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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. Chatterjee S, Mizar P, Cassel R, Neidl R, Selvi BR, Mohankrishna DV, Vedamurthy BM, Schneider A, Bousiges O, Mathis C et al.. (2013) A novel activator of CBP/p300 acetyltransferases promotes neurogenesis and extends memory duration in adult mice. J Neurosci, 33 (26): 10698-712. [PMID:23804093]
3. Chen Z, Wang M, Wu D, Bai L, Xu T, Metwally H, Wang Y, McEachern D, Zhao L, Li R et al.. (2024) Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression. J Med Chem, [Epub ahead of print]. [PMID:38477974]
4. Chen Z, Wang M, Wu D, Zhao L, Metwally H, Jiang W, Wang Y, Bai L, McEachern D, Luo J et al.. (2024) Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer. J Med Chem, 67 (7): 5351-5372. [PMID:38530938]
5. 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]
6. Gallenkamp D, Gelato KA, Haendler B, Weinmann H. (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem, 9 (3): 438-64. [PMID:24497428]
7. Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW et al.. (2017) GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem, 60 (22): 9162-9183. [PMID:28892380]
8. 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]
9. SGC. I-CBP112 A CREBBP/EP300-selective chemical probe. Accessed on 04/08/2023. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/I-CBP112
10. Welti J, Sharp A, Brooks N, Yuan W, McNair C, Chand SN, Pal A, Figueiredo I, Riisnaes R, Gurel B et al.. (2021) Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov, 11 (5): 1118-1137. [PMID:33431496]
11. Xiang Q, Wang C, Wu T, Zhang C, Hu Q, Luo G, Hu J, Zhuang X, Zou L, Shen H et al.. (2022) Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. J Med Chem, 65 (1): 785-810. [PMID:34962793]
Non-enzymatic BRD containing proteins: CREB binding protein. Last modified on 02/04/2024. Accessed on 04/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2734.