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bromodomain testis associated

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Target id: 2729

Nomenclature: bromodomain testis associated

Family: Non-enzymatic BRD containing proteins

Contents:

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
Alphafold Q58F21 (Hs), Q91Y44 (Mm)
CATH/Gene3D 1.20.920.10
ChEMBL Target CHEMBL1795185 (Hs)
Ensembl Gene ENSG00000137948 (Hs), ENSMUSG00000029279 (Mm), ENSRNOG00000002073 (Rn)
Entrez Gene 676 (Hs), 114642 (Mm), 305123 (Rn)
Human Protein Atlas ENSG00000137948 (Hs)
KEGG Gene hsa:676 (Hs), mmu:114642 (Mm), rno:305123 (Rn)
OMIM 602144 (Hs)
Pharos Q58F21 (Hs)
RefSeq Nucleotide NM_001242806 (Hs), NM_054054 (Mm), NM_001012031 (Rn)
RefSeq Protein NP_001229735 (Hs), NP_473395 (Mm), NP_001012031 (Rn)
UniProtKB Q58F21 (Hs), Q91Y44 (Mm)
Wikipedia BRDT (Hs)
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:  3

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
GSK852 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.8 – 8.8 pKd 1
⤷ pKd 8.8 (Kd 1.58x10-9 M) [1]
Description: Binding affinity at BD2, determined by BROMOscan
pKd 4.8 (Kd 1.585x10-5 M) [1]
Description: Binding affinity at BD1, determined by BROMOscan
XD14 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 pKd 2
⤷ pKd 5.9 (Kd 1.2x10-6 M) [2]
Description: Assay using recombinant BRDT-BD1.
(+)-JQ1 Small molecule or natural product Mm Inhibition 8.0 pIC50 3
⤷ pIC50 8.0 (IC50 1x10-8 M) [3]
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 3
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [3]
Description: Inhibition of H4Kac4 binding to hBRDT-BD1
WNY0824 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.5 pIC50 4
⤷ pIC50 6.5 (IC50 3.12x10-7 M) [4]
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 SCC, Atkinson SJ, Chung CW, Davis R, Gordon L, Grandi P, Gray JJR, Grimes T, Phillipou A, Preston AG et al.. (2021) Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors. J Med Chem, 64 (15): 10711-10741. [PMID:34260229]

2. 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]

3. 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]

4. Wang NY, Xu Y, Xiao KJ, Zuo WQ, Zhu YX, Hu R, Wang WL, Shi YJ, Yu LT, Liu ZH. (2020) Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. Eur J Med Chem, 191: 112152. [PMID:32088495]

How to cite this page

Non-enzymatic BRD containing proteins: bromodomain testis associated. Last modified on 23/08/2022. Accessed on 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2729.