Details of the Target

General Information of Target

Target ID LDTP11563
Target Name Forkhead box protein P3 (FOXP3)
Gene Name FOXP3
Gene ID 50943
Synonyms
IPEX; Forkhead box protein P3; Scurfin) [Cleaved into: Forkhead box protein P3, C-terminally processed; Forkhead box protein P3 41 kDa form]
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MAENWKNCFEEELICPICLHVFVEPVQLPCKHNFCRGCIGEAWAKDSGLVRCPECNQAYN
QKPGLEKNLKLTNIVEKFNALHVEKPPAALHCVFCRRGPPLPAQKVCLRCEAPCCQSHVQ
THLQQPSTARGHLLVEADDVRAWSCPQHNAYRLYHCEAEQVAVCQYCCYYSGAHQGHSVC
DVEIRRNEIRKMLMKQQDRLEEREQDIEDQLYKLESDKRLVEEKVNQLKEEVRLQYEKLH
QLLDEDLRQTVEVLDKAQAKFCSENAAQALHLGERMQEAKKLLGSLQLLFDKTEDVSFMK
NTKSVKILMDRTQTCTSSSLSPTKIGHLNSKLFLNEVAKKEKQLRKMLEGPFSTPVPFLQ
SVPLYPCGVSSSGAEKRKHSTAFPEASFLETSSGPVGGQYGAAGTASGEGQSGQPLGPCS
STQHLVALPGGAQPVHSSPVFPPSQYPNGSAAQQPMLPQYGGRKILVCSVDNCYCSSVAN
HGGHQPYPRSGHFPWTVPSQEYSHPLPPTPSVPQSLPSLAVRDWLDASQQPGHQDFYRVY
GQPSTKHYVTS
Target Type
Clinical trial
Target Bioclass
Transcription factor
Subcellular location
Nucleus
Function
Transcriptional regulator which is crucial for the development and inhibitory function of regulatory T-cells (Treg). Plays an essential role in maintaining homeostasis of the immune system by allowing the acquisition of full suppressive function and stability of the Treg lineage, and by directly modulating the expansion and function of conventional T-cells. Can act either as a transcriptional repressor or a transcriptional activator depending on its interactions with other transcription factors, histone acetylases and deacetylases. The suppressive activity of Treg involves the coordinate activation of many genes, including CTLA4 and TNFRSF18 by FOXP3 along with repression of genes encoding cytokines such as interleukin-2 (IL2) and interferon-gamma (IFNG). Inhibits cytokine production and T-cell effector function by repressing the activity of two key transcription factors, RELA and NFATC2. Mediates transcriptional repression of IL2 via its association with histone acetylase KAT5 and histone deacetylase HDAC7. Can activate the expression of TNFRSF18, IL2RA and CTLA4 and repress the expression of IL2 and IFNG via its association with transcription factor RUNX1. Inhibits the differentiation of IL17 producing helper T-cells (Th17) by antagonizing RORC function, leading to down-regulation of IL17 expression, favoring Treg development. Inhibits the transcriptional activator activity of RORA. Can repress the expression of IL2 and IFNG via its association with transcription factor IKZF4.
TTD ID
T36958
Uniprot ID
Q9BZS1
DrugMap ID
TT1X3QF
Ensemble ID
ENST00000376199.7
HGNC ID
HGNC:6106

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HT29 SNV: p.P177H .
JURKAT Deletion: p.P302LfsTer88 .
PC9 Substitution: p.M64_P65delinsIT .
WM2664 Insertion: p.T135HfsTer71; p.A404GfsTer7 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C280(14.63)  LDD1704  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell-activated C280(14.63)  LDD1704  [1]
 LDCM0024  KB05 T cell-activated C169(8.22)  LDD1706  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone deacetylase 7 (HDAC7) Histone deacetylase family Q8WUI4
Histone acetyltransferase KAT5 (KAT5) MYST (SAS/MOZ) family Q92993
Ubiquitin carboxyl-terminal hydrolase 44 (USP44) Peptidase C19 family Q9H0E7
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit (PPP1CA) PPP phosphatase family P62136
E3 ubiquitin-protein ligase CHIP (STUB1) . Q9UNE7
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein FosB (FOSB) BZIP family P53539
Zinc finger protein Aiolos (IKZF3) Ikaros C2H2-type zinc-finger protein family Q9UKT9
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin-associated protein 3-3 (KRTAP3-3) KRTAP type 3 family Q9BYR6
Keratin-associated protein 6-2 (KRTAP6-2) KRTAP type 6 family Q3LI66
Keratin-associated protein 8-1 (KRTAP8-1) KRTAP type 8 family Q8IUC2
Proline-rich protein 20C (PRR20C) PRR20 family P86479
Proline-rich protein 20D (PRR20D) PRR20 family P86480
Proline-rich protein 20E (PRR20E) PRR20 family P86478
RNA-binding protein with multiple splicing (RBPMS) . Q93062

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd8701 Antisense oligonucleotide DX9T0N

References

1 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.