tripartite motif containing 24 | TIF1 family | IUPHAR/BPS Guide to PHARMACOLOGY

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tripartite motif containing 24

Target not currently curated in GtoImmuPdb

Target id: 2252

Nomenclature: tripartite motif containing 24

Abbreviated Name: TIF1A

Family: TIF1 family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1016 7q32-q34 TRIM24 tripartite motif containing 24
Mouse - 1051 6 B1 Trim24 tripartite motif-containing 24
Rat - 866 4 q22 Trim24 tripartite motif-containing 24
Previous and Unofficial Names
ab2-427 | TIF1 | TIF1alpha | transcription intermediary factor 1-alpha
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of TRIM24 PHD-Bromo in the free state.
PDB Id:  3O33
Resolution:  2.0Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of TRIM24 PHD-Bromo complexed with H4(14-19)K16ac peptide.
PDB Id:  3O36
Resolution:  1.7Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor.
PDB Id:  4ZQL
Ligand:  compound 34 [PMID: 25974391]
Resolution:  1.79Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 6.3.2.-

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 Value Parameter Reference
compound 34 [PMID: 25974391] Hs Binding 6.7 pKd 1
pKd 6.7 (Kd 2.22x10-7 M) [1]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
dTRIM24 Hs Binding 6.5 pIC50 2
pIC50 6.5 (IC50 3.377x10-7 M) [2]
Description: Active binding to the TRIM24 bromodomain in TRIM24 ligand-displacement (AlphaScreen) assay.
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Rara+|Raratm3.1Ipc|Trim24tm1.1Los Raratm3.1Ipc/Rara+,Trim24tm1.1Los/Trim24tm1.1Los
involves: 129/Sv * C57BL/6 * SJL
MGI:109275  MGI:97856  MP:0003893 increased hepatocyte proliferation PMID: 18026104 
Raratm3Ipc|Tg(Alb-cre)21Mgn|Trim24tm1Los Raratm3Ipc/Raratm3Ipc,Tg(Alb-cre)21Mgn/?,Trim24tm1Los/Trim24tm1Los
involves: 129/Sv * C57BL/6 * DBA * SJL
MGI:109275  MGI:2176226  MGI:97856  MP:0003893 increased hepatocyte proliferation PMID: 18026104 
Rara+|Raratm3Ipc|Tg(Alb-cre)21Mgn|Trim24tm1Los Raratm3Ipc/Rara+,Tg(Alb-cre)21Mgn/?,Trim24tm1Los/Trim24tm1Los
involves: 129/Sv * C57BL/6 * DBA * SJL
MGI:109275  MGI:2176226  MGI:97856  MP:0003893 increased hepatocyte proliferation PMID: 18026104 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Thyroid carcinoma, papillary
Synonyms: Differentiated thyroid carcinoma [Orphanet: ORPHA146]
Papillary thyroid carcinoma [Disease Ontology: DOID:3969]
Disease Ontology: DOID:3969
OMIM: 188550
Orphanet: ORPHA146

References

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1. Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C et al.. (2016) Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. J. Med. Chem., 59 (4): 1642-7. [PMID:25974391]

2. Gechijian LN, Buckley DL, Lawlor MA, Reyes JM, Paulk J, Ott CJ, Winter GE, Erb MA, Scott TG, Xu M et al.. (2018) Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat. Chem. Biol., 14 (4): 405-412. [PMID:29507391]

3. Tsai WW, Wang Z, Yiu TT, Akdemir KC, Xia W, Winter S, Tsai CY, Shi X, Schwarzer D, Plunkett W et al.. (2010) TRIM24 links a non-canonical histone signature to breast cancer. Nature, 468 (7326): 927-32. [PMID:21164480]

How to cite this page

TIF1 family: tripartite motif containing 24. Last modified on 08/11/2019. Accessed on 16/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2252.