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tripartite motif containing 24

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Target not currently curated in GtoImmuPdb

Target id: 2252

Nomenclature: tripartite motif containing 24

Abbreviated Name: TIF1A

Family: TIF1 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1050 7q33-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 Click here for help
ab2-427 | TIF1 | TIF1alpha | transcription intermediary factor 1-alpha
Database Links Click here for help
Alphafold O15164 (Hs), Q64127 (Mm)
BRENDA 6.3.2.-
CATH/Gene3D 1.20.920.10, 3.30.40.10
ChEMBL Target CHEMBL3108638 (Hs)
Ensembl Gene ENSG00000122779 (Hs), ENSMUSG00000029833 (Mm), ENSRNOG00000013251 (Rn)
Entrez Gene 8805 (Hs), 21848 (Mm), 500084 (Rn)
Human Protein Atlas ENSG00000122779 (Hs)
KEGG Enzyme 6.3.2.-
KEGG Gene hsa:8805 (Hs), mmu:21848 (Mm), rno:500084 (Rn)
OMIM 603406 (Hs)
Orphanet ORPHA120263 (Hs)
Pharos O15164 (Hs)
RefSeq Nucleotide NM_003852 (Hs), NM_145076 (Mm), NM_001044266 (Rn)
RefSeq Protein NP_003843 (Hs), NP_659542 (Mm), NP_001037731 (Rn)
UniProtKB O15164 (Hs), Q64127 (Mm)
Wikipedia TRIM24 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 6.3.2.-

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
compound 34 [PMID: 25974391] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure 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 Small molecule or natural product 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.
Immuno Process Associations
Immuno Process:  Cellular signalling
Phenotypes, Alleles and Disease Models Click here for help 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 Click here for help
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 05/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2252.