bromodomain containing 7 | Bromodomain kinase (BRDK) family | IUPHAR/BPS Guide to PHARMACOLOGY

bromodomain containing 7

Target id: 2726

Nomenclature: bromodomain containing 7

Abbreviated Name: BRD7

Family: Bromodomain kinase (BRDK) family

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 :     Currently no data for bromodomain containing 7 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 652 16q12.1 BRD7 bromodomain containing 7
Mouse - 651 8 C4 Brd7 bromodomain containing 7
Rat - 406 19p11 Brd7 bromodomain containing 7
Previous and Unofficial Names
BP75 | CELTIX1
Database Links
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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
BI-9564 Hs Inhibition 6.6 pKd 4
pKd 6.6 (Kd 2.39x10-7 M) [4]
LP99 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 Hs Inhibition 6.5 pIC50 3
pIC50 6.5 (IC50 3.4x10-7 M) [3]
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

Show »

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

4. Structural Genomics Consortium. BI-9564 A chemical probe for BRD9 and BRD7. Accessed on 11/12/2015. Modified on 11/12/2015. The Structural Genomics Consortium, http://www.thesgc.org/chemical-probes/BI-9564

How to cite this page

Bromodomain kinase (BRDK) family: bromodomain containing 7. Last modified on 05/04/2017. Accessed on 19/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2726.