ATPase family, AAA domain containing 2

Target id: 2719

Nomenclature: ATPase family, AAA domain containing 2

Family: 3.6.1.3 ATPases

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 ATPase family, AAA domain containing 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1390 8q24.13 ATAD2 ATPase family, AAA domain containing 2
Mouse - 1364 15 D2 Atad2 ATPase family, AAA domain containing 2
Rat - 1373 7q33 Atad2 ATPase family, AAA domain containing 2
Previous and Unofficial Names
ATPase family
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human ATAD2 bromodomain in complex with 5-5- methoxypyridin-3-yl-3-methyl-8-piperidin-4-ylamino-1,2-dihydro-1,7- naphthyridin-2-one (compound 60).
PDB Id:  5A5R
Ligand:  compound 60 [PMID: 26155854]
Resolution:  2.01Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human ATAD2 bromodomain in complex with 4-(3R,4R) -4-(3-methyl-2-oxo-1,2-dihydro-1,7-naphthyridin-8-yl)aminopiperidin-3- yloxymethyl)-1-thiane-1,1-dione
PDB Id:  5A82
Ligand:  compound 33 [PMID: 26230603]
Resolution:  1.86Å
Species:  Human
References:  2
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human ATAD2 bromodomain in complex with 8-(((3R,4R,5S)-3-((4,4-difluorocyclohexyl)methoxy)-5-methoxypiperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one.
PDB Id:  5LJ0
Ligand:  GSK8814
Resolution:  1.82Å
Species:  Human
References:  1
Enzyme Reaction
EC Number: 3.6.1.3

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
GSK8814 Hs Inhibition 8.1 pKd 1
pKd 8.1 (Kd 8x10-9 M) [1]
Description: By isothermal titration calorimetry (ICT) assay.
GSK8814 Hs Inhibition 8.9 pKi 1
pKi 8.9 (Ki 1.25x10-9 M) [1]
Description: By Bromosphere assay using full length endogenous protein.
GSK8814 Hs Inhibition 7.3 pIC50 1
pIC50 7.3 (IC50 5.01x10-8 M) [1]
Description: By TR-FRET assay.
compound 57 [PMID: 26155854] Hs Inhibition 5.9 pIC50 3
pIC50 5.9 [3]
compound 60 [PMID: 26155854] Hs Inhibition 5.9 pIC50 3
pIC50 5.9 [3]
compound 33 [PMID: 26230603] Hs Inhibition 5.3 pIC50 2
pIC50 5.3 [2]
General Comments
This is a bromo-domain containing protein involved in chromatin modification.

References

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1. Bamborough P, Chung CW, Demont EH, Furze RC, Bannister AJ, Che KH, Diallo H, Douault C, Grandi P, Kouzarides T et al.. (2016) A Chemical Probe for the ATAD2 Bromodomain. Angew. Chem. Int. Ed. Engl.55 (38): 11382-6. [PMID:27530368]

2. Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C et al.. (2015) Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. J. Med. Chem.58 (15): 6151-78. [PMID:26230603]

3. Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H et al.. (2015) Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors. J. Med. Chem.58 (14): 5649-73. [PMID:26155854]

How to cite this page

3.6.1.3 ATPases: ATPase family, AAA domain containing 2. Last modified on 05/04/2017. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2719.