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bromodomain containing 7

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Target not currently curated in GtoImmuPdb

Target id: 2726

Nomenclature: bromodomain containing 7

Abbreviated Name: BRD7

Family: Bromodomain kinase (BRDK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 651 16q12.1 BRD7 bromodomain containing 7
Mouse - 651 8 C3 Brd7 bromodomain containing 7
Rat - 406 19p11 Brd7 bromodomain containing 7
Previous and Unofficial Names Click here for help
BP75 | CELTIX1
Database Links Click here for help
Alphafold Q9NPI1 (Hs), O88665 (Mm)
CATH/Gene3D 1.20.920.10
ChEMBL Target CHEMBL3085622 (Hs), CHEMBL3822348 (Mm)
Ensembl Gene ENSG00000166164 (Hs), ENSMUSG00000031660 (Mm), ENSRNOG00000014419 (Rn)
Entrez Gene 29117 (Hs), 26992 (Mm), 361374 (Rn)
Human Protein Atlas ENSG00000166164 (Hs)
KEGG Gene hsa:29117 (Hs), mmu:26992 (Mm), rno:361374 (Rn)
Pharos Q9NPI1 (Hs)
RefSeq Nucleotide NM_001173984 (Hs), NM_012047 (Mm), NM_001108440 (Rn)
RefSeq Protein NP_001167455 (Hs), NP_036177 (Mm), NP_001101910 (Rn)
UniProtKB Q9NPI1 (Hs), O88665 (Mm)
Wikipedia BRD7 (Hs)

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BI-9564 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pKd 3
⤷ pKd 6.6 (Kd 2.39x10-7 M) [3]
LP99 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition ~6.0 pKd 1
⤷ pKd ~6.0 (Kd ~1x10-6 M) [1]
Description: Based on binding of BRD7 being 10-fold lower than for BRD9
TP-472 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.5 pIC50 4
⤷ pIC50 6.5 (IC50 3.4x10-7 M) [4]
Description: By isothermal titration calorimetry (ITC).
General Comments
BRD7 suppresses tumorigenicity by serving as a p53 cofactor required for the efficient induction of p53-dependent oncogene-induced senescence. This appears to be mediated by physical interaction between residues in the C-terminal domain of p53 and amino-terminal region of BRD7 [2].

References

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1. Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S et al.. (2015) LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl, 54 (21): 6217-21. [PMID:25864491]

2. Drost J, Mantovani F, Tocco F, Elkon R, Comel A, Holstege H, Kerkhoven R, Jonkers J, Voorhoeve PM, Agami R et al.. (2010) BRD7 is a candidate tumour suppressor gene required for p53 function. Nat Cell Biol, 12 (4): 380-9. [PMID:20228809]

3. SCC. BI-9564 A chemical probe for BRD9 and BRD7. Accessed on 11/12/2015. Modified on 11/12/2015. thesgc.org, http://www.thesgc.org/chemical-probes/BI-9564

4. SGC. TP-472 A BRD9/7 Probe. Accessed on 05/04/2017. Modified on 04/08/2023. Structural Genomics Consortium., https://www.thesgc.org/chemical-probes/TP-472

How to cite this page

Bromodomain kinase (BRDK) family: bromodomain containing 7. Last modified on 05/04/2017. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2726.