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bromodomain testis associated

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Target not currently curated in GtoImmuPdb

Target id: 2729

Nomenclature: bromodomain testis associated

Family: Non-enzymatic BRD containing proteins

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 947 1p22.1 BRDT bromodomain testis associated
Mouse - 956 5 E5 Brdt bromodomain, testis-specific
Rat - 326 14p22 Brdt bromodomain testis associated
Previous and Unofficial Names Click here for help
BRD6 | CT9 | cancer/testis antigen 9 | bromodomain, testis-specific | bromodomain
Database Links Click here for help
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the first bromodomain of human BRDT in complex with the inhibitor JQ1
PDB Id:  4FLP
Ligand:  (+)-JQ1
Resolution:  2.23Å
Species:  Human
References:  2

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
XD14 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 pKd 1
pKd 5.9 (Kd 1.2x10-6 M) [1]
Description: Assay using recombinant BRDT-BD1.
(+)-JQ1 Small molecule or natural product Mm Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1x10-8 M) [2]
Description: Inhibition of H4Kac4 binding to mBRDT-BD1
(+)-JQ1 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1.1x10-8 M) [2]
Description: Inhibition of H4Kac4 binding to hBRDT-BD1
View species-specific inhibitor tables
Inhibitor Comments
(+)-JQ1 inhibits BET family epigenetic reader proteins, such as BRD4 and BRDT.

References

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1. Lucas X, Wohlwend D, Hügle M, Schmidtkunz K, Gerhardt S, Schüle R, Jung M, Einsle O, Günther S. (2013) 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew. Chem. Int. Ed. Engl., 52 (52): 14055-9. [PMID:24272870]

2. Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, Lemieux ME, Picaud S, Yu RN, Qi J et al.. (2012) Small-molecule inhibition of BRDT for male contraception. Cell, 150 (4): 673-84. [PMID:22901802]

How to cite this page

Non-enzymatic BRD containing proteins: bromodomain testis associated. Last modified on 13/02/2017. Accessed on 04/12/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2729.