Details of the Target

General Information of Target

Target ID LDTP13919
Target Name Thyroid hormone receptor-associated protein 3 (THRAP3)
Gene Name THRAP3
Gene ID 9967
Synonyms
BCLAF2; TRAP150; Thyroid hormone receptor-associated protein 3; BCLAF1 and THRAP3 family member 2; Thyroid hormone receptor-associated protein complex 150 kDa component; Trap150
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAEGSGEVVAVSATGAANGLNNGAGGTSATTCNPLSRKLHKILETRLDNDKEMLEALKAL
STFFVENSLRTRRNLRGDIERKSLAINEEFVSIFKEVKEELESISEDVQAMSNCCQDMTS
RLQAAKEQTQDLIVKTTKLQSESQKLEIRAQVADAFLSKFQLTSDEMSLLRGTREGPITE
DFFKALGRVKQIHNDVKVLLRTNQQTAGLEIMEQMALLQETAYERLYRWAQSECRTLTQE
SCDVSPVLTQAMEALQDRPVLYKYTLDEFGTARRSTVVRGFIDALTRGGPGGTPRPIEMH
SHDPLRYVGDMLAWLHQATASEKEHLEALLKHVTTQGVEENIQEVVGHITEGVCRPLKVR
IEQVIVAEPGAVLLYKISNLLKFYHHTISGIVGNSATALLTTIEEMHLLSKKIFFNSLSL
HASKLMDKVELPPPDLGPSSALNQTLMLLREVLASHDSSVVPLDARQADFVQVLSCVLDP
LLQMCTVSASNLGTADMATFMVNSLYMMKTTLALFEFTDRRLEMLQFQIEAHLDTLINEQ
ASYVLTRVGLSYIYNTVQQHKPEQGSLANMPNLDSVTLKAAMVQFDRYLSAPDNLLIPQL
NFLLSATVKEQIVKQSTELVCRAYGEVYAAVMNPINEYKDPENILHRSPQQVQTLLS
Target Bioclass
Other
Family
BCLAF1/THRAP3 family
Subcellular location
Nucleus
Function
Involved in pre-mRNA splicing. Remains associated with spliced mRNA after splicing which probably involves interactions with the exon junction complex (EJC). Can trigger mRNA decay which seems to be independent of nonsense-mediated decay involving premature stop codons (PTC) recognition. May be involved in nuclear mRNA decay. Involved in regulation of signal-induced alternative splicing. During splicing of PTPRC/CD45 is proposed to sequester phosphorylated SFPQ from PTPRC/CD45 pre-mRNA in resting T-cells. Involved in cyclin-D1/CCND1 mRNA stability probably by acting as component of the SNARP complex which associates with both the 3'end of the CCND1 gene and its mRNA. Involved in response to DNA damage. Is excluced from DNA damage sites in a manner that parallels transcription inhibition; the function may involve the SNARP complex. Initially thought to play a role in transcriptional coactivation through its association with the TRAP complex; however, it is not regarded as a stable Mediator complex subunit. Cooperatively with HELZ2, enhances the transcriptional activation mediated by PPARG, maybe through the stabilization of the PPARG binding to DNA in presence of ligand. May play a role in the terminal stage of adipocyte differentiation. Plays a role in the positive regulation of the circadian clock. Acts as a coactivator of the CLOCK-BMAL1 heterodimer and promotes its transcriptional activator activity and binding to circadian target genes.
Uniprot ID
Q9Y2W1
Ensemble ID
ENST00000354618.10
HGNC ID
HGNC:22964
ChEMBL ID
CHEMBL4105820

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 24 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		11.07  LDD0402  [1]
P3
 Probe Info  		1.77  LDD0450  [2]
A-EBA
 Probe Info  		3.28  LDD0215  [3]
CY-1
 Probe Info  		100.00  LDD0243  [4]
TH211
 Probe Info  		Y54(9.30)  LDD0260  [5]
C-Sul
 Probe Info  		2.73  LDD0066  [6]
ONAyne
 Probe Info  		N.A.  LDD0273  [7]
OPA-S-S-alkyne
 Probe Info  		K486(1.70); K711(1.73); K346(2.43); K519(3.80)  LDD3494  [8]
Probe 1
 Probe Info  		Y344(24.66); Y710(33.62)  LDD3495  [9]
DBIA
 Probe Info  		C476(1.54)  LDD2248  [10]
HHS-475
 Probe Info  		Y710(0.49); Y880(0.74); Y228(2.26)  LDD0264  [11]
HHS-465
 Probe Info  		Y228(10.00)  LDD2237  [12]
5E-2FA
 Probe Info  		N.A.  LDD2235  [13]
ATP probe
 Probe Info  		K551(0.00); K221(0.00); K697(0.00); K527(0.00)  LDD0199  [14]
NHS
 Probe Info  		K811(0.00); K709(0.00); K221(0.00); K688(0.00)  LDD0010  [15]
SF
 Probe Info  		Y228(0.00); Y710(0.00); Y873(0.00); Y344(0.00)  LDD0028  [16]
STPyne
 Probe Info  		N.A.  LDD0009  [15]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [17]
Ox-W18
 Probe Info  		W223(0.00); W471(0.00); W869(0.00)  LDD2175  [18]
1c-yne
 Probe Info  		K215(0.00); K221(0.00)  LDD0228  [19]
1d-yne
 Probe Info  		N.A.  LDD0357  [19]
Acrolein
 Probe Info  		H637(0.00); H883(0.00); H689(0.00); H636(0.00)  LDD0217  [20]
Crotonaldehyde
 Probe Info  		H613(0.00); H58(0.00); H651(0.00); H883(0.00)  LDD0219  [20]
HHS-482
 Probe Info  		Y228(1.37); Y344(0.83); Y710(1.07); Y873(0.77)  LDD2239  [12]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C187
 Probe Info  		18.90  LDD1865  [21]
C191
 Probe Info  		13.00  LDD1868  [21]
C193
 Probe Info  		5.58  LDD1869  [21]
FFF probe13
 Probe Info  		20.00  LDD0475  [22]
Diazir
 Probe Info  		N.A.  LDD0011  [15]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 11.39  LDD0403  [1]
 LDCM0108  Chloroacetamide HeLa H689(0.00); H637(0.00); H641(0.00); H613(0.00)  LDD0222  [20]
 LDCM0116  HHS-0101 DM93 Y710(0.49); Y880(0.74); Y228(2.26)  LDD0264  [11]
 LDCM0117  HHS-0201 DM93 Y228(1.80); Y344(20.00)  LDD0265  [11]
 LDCM0118  HHS-0301 DM93 Y880(1.20); Y344(7.69)  LDD0266  [11]
 LDCM0119  HHS-0401 DM93 Y880(0.51); Y344(0.67); Y228(2.28)  LDD0267  [11]
 LDCM0120  HHS-0701 DM93 Y880(0.56); Y228(1.05)  LDD0268  [11]
 LDCM0107  IAA HeLa H613(0.00); H637(0.00); H689(0.00); H636(0.00)  LDD0221  [20]
 LDCM0022  KB02 8305C C476(1.54)  LDD2248  [10]
 LDCM0023  KB03 8505C C476(1.58)  LDD2666  [10]
 LDCM0024  KB05 CAL-62 C476(2.64)  LDD3123  [10]
 LDCM0109  NEM HeLa H637(0.00); H613(0.00); H58(0.00); H883(0.00)  LDD0223  [20]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Eukaryotic initiation factor 4A-III (EIF4A3) DEAD box helicase family P38919
Casein kinase II subunit alpha (CSNK2A1) Ser/Thr protein kinase family P68400
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear RNA export factor 1 (NXF1) NXF family Q9UBU9
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Splicing factor, proline- and glutamine-rich (SFPQ) . P23246
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
SNW domain-containing protein 1 (SNW1) SNW family Q13573

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
3 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
5 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
6 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
7 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
8 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
9 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
10 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
11 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
12 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
13 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
14 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
15 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
16 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
17 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
18 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
19 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
20 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
21 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
22 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.