General Information of Target

Target ID LDTP04701
Target Name Hepatocyte nuclear factor 3-alpha (FOXA1)
Gene Name FOXA1
Gene ID 3169
Synonyms
HNF3A; TCF3A; Hepatocyte nuclear factor 3-alpha; HNF-3-alpha; HNF-3A; Forkhead box protein A1; Transcription factor 3A; TCF-3A
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLGTVKMEGHETSDWNSYYADTQEAYSSVPVSNMNSGLGSMNSMNTYMTMNTMTTSGNMT
PASFNMSYANPGLGAGLSPGAVAGMPGGSAGAMNSMTAAGVTAMGTALSPSGMGAMGAQQ
AASMNGLGPYAAAMNPCMSPMAYAPSNLGRSRAGGGGDAKTFKRSYPHAKPPYSYISLIT
MAIQQAPSKMLTLSEIYQWIMDLFPYYRQNQQRWQNSIRHSLSFNDCFVKVARSPDKPGK
GSYWTLHPDSGNMFENGCYLRRQKRFKCEKQPGAGGGGGSGSGGSGAKGGPESRKDPSGA
SNPSADSPLHRGVHGKTGQLEGAPAPGPAASPQTLDHSGATATGGASELKTPASSTAPPI
SSGPGALASVPASHPAHGLAPHESQLHLKGDPHYSFNHPFSINNLMSSSEQQHKLDFKAY
EQALQYSPYGSTLPASLPLGSASVTTRSPIEPSALEPAYYQGVYSRPVLNTS
Target Bioclass
Transcription factor
Subcellular location
Nucleus
Function
Transcription factor that is involved in embryonic development, establishment of tissue-specific gene expression and regulation of gene expression in differentiated tissues. Is thought to act as a 'pioneer' factor opening the compacted chromatin for other proteins through interactions with nucleosomal core histones and thereby replacing linker histones at target enhancer and/or promoter sites. Binds DNA with the consensus sequence 5'-[AC]A[AT]T[AG]TT[GT][AG][CT]T[CT]-3'. Proposed to play a role in translating the epigenetic signatures into cell type-specific enhancer-driven transcriptional programs. Its differential recruitment to chromatin is dependent on distribution of histone H3 methylated at 'Lys-5' (H3K4me2) in estrogen-regulated genes. Involved in the development of multiple endoderm-derived organ systems such as liver, pancreas, lung and prostate; FOXA1 and FOXA2 seem to have at least in part redundant roles. Modulates the transcriptional activity of nuclear hormone receptors. Is involved in ESR1-mediated transcription; required for ESR1 binding to the NKX2-1 promoter in breast cancer cells; binds to the RPRM promoter and is required for the estrogen-induced repression of RPRM. Involved in regulation of apoptosis by inhibiting the expression of BCL2. Involved in cell cycle regulation by activating expression of CDKN1B, alone or in conjunction with BRCA1. Originally described as a transcription activator for a number of liver genes such as AFP, albumin, tyrosine aminotransferase, PEPCK, etc. Interacts with the cis-acting regulatory regions of these genes. Involved in glucose homeostasis.
Uniprot ID
P55317
Ensemble ID
ENST00000250448.5
HGNC ID
HGNC:5021

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO678 SNV: p.S331R .
DU145 Deletion: p.A340RfsTer10 .
MEWO SNV: p.S40F; p.D249N .
MOLT4 SNV: p.A133T .
OCIAML2 SNV: p.G378S .
OVKATE SNV: p.A20S .
SG231 SNV: p.G275S .
SKNSH SNV: p.P110T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C258(1.43)  LDD0078  [1]
IA-alkyne
 Probe Info 
C227(0.00); C258(0.00)  LDD0162  [2]
TFBX
 Probe Info 
N.A.  LDD0148  [3]
NAIA_5
 Probe Info 
C268(0.00); C227(0.00); C258(0.00)  LDD2223  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C258(1.11)  LDD1507  [5]
 LDCM0226  AC11 HEK-293T C258(0.93)  LDD1509  [5]
 LDCM0237  AC12 HEK-293T C258(1.01)  LDD1510  [5]
 LDCM0259  AC14 HEK-293T C258(0.83)  LDD1512  [5]
 LDCM0276  AC17 HEK-293T C258(1.00)  LDD1515  [5]
 LDCM0278  AC19 HEK-293T C258(0.84)  LDD1517  [5]
 LDCM0280  AC20 HEK-293T C258(1.18)  LDD1519  [5]
 LDCM0281  AC21 HEK-293T C258(1.05)  LDD1520  [5]
 LDCM0282  AC22 HEK-293T C258(0.75)  LDD1521  [5]
 LDCM0284  AC24 HEK-293T C258(1.02)  LDD1523  [5]
 LDCM0285  AC25 HEK-293T C258(0.96)  LDD1524  [5]
 LDCM0287  AC27 HEK-293T C258(1.08)  LDD1526  [5]
 LDCM0288  AC28 HEK-293T C258(0.98)  LDD1527  [5]
 LDCM0289  AC29 HEK-293T C258(1.39)  LDD1528  [5]
 LDCM0290  AC3 HEK-293T C258(1.11)  LDD1529  [5]
 LDCM0291  AC30 HEK-293T C258(0.84)  LDD1530  [5]
 LDCM0293  AC32 HEK-293T C258(1.17)  LDD1532  [5]
 LDCM0294  AC33 HEK-293T C258(1.12)  LDD1533  [5]
 LDCM0296  AC35 HEK-293T C258(1.00)  LDD1535  [5]
 LDCM0297  AC36 HEK-293T C258(1.11)  LDD1536  [5]
 LDCM0298  AC37 HEK-293T C258(1.15)  LDD1537  [5]
 LDCM0299  AC38 HEK-293T C258(0.80)  LDD1538  [5]
 LDCM0301  AC4 HEK-293T C258(1.00)  LDD1540  [5]
 LDCM0302  AC40 HEK-293T C258(1.02)  LDD1541  [5]
 LDCM0303  AC41 HEK-293T C258(1.10)  LDD1542  [5]
 LDCM0305  AC43 HEK-293T C258(1.09)  LDD1544  [5]
 LDCM0306  AC44 HEK-293T C258(1.31)  LDD1545  [5]
 LDCM0307  AC45 HEK-293T C258(1.13)  LDD1546  [5]
 LDCM0308  AC46 HEK-293T C258(1.03)  LDD1547  [5]
 LDCM0310  AC48 HEK-293T C258(1.06)  LDD1549  [5]
 LDCM0311  AC49 HEK-293T C258(0.92)  LDD1550  [5]
 LDCM0312  AC5 HEK-293T C258(1.51)  LDD1551  [5]
 LDCM0314  AC51 HEK-293T C258(0.96)  LDD1553  [5]
 LDCM0315  AC52 HEK-293T C258(1.27)  LDD1554  [5]
 LDCM0316  AC53 HEK-293T C258(1.39)  LDD1555  [5]
 LDCM0317  AC54 HEK-293T C258(1.13)  LDD1556  [5]
 LDCM0319  AC56 HEK-293T C258(1.03)  LDD1558  [5]
 LDCM0320  AC57 HEK-293T C258(1.24)  LDD1559  [5]
 LDCM0322  AC59 HEK-293T C258(1.13)  LDD1561  [5]
 LDCM0323  AC6 HEK-293T C258(0.90)  LDD1562  [5]
 LDCM0324  AC60 HEK-293T C258(0.91)  LDD1563  [5]
 LDCM0325  AC61 HEK-293T C258(1.02)  LDD1564  [5]
 LDCM0326  AC62 HEK-293T C258(1.10)  LDD1565  [5]
 LDCM0328  AC64 HEK-293T C258(0.99)  LDD1567  [5]
 LDCM0345  AC8 HEK-293T C258(1.30)  LDD1569  [5]
 LDCM0248  AKOS034007472 HEK-293T C258(1.13)  LDD1511  [5]
 LDCM0356  AKOS034007680 HEK-293T C258(1.18)  LDD1570  [5]
 LDCM0275  AKOS034007705 HEK-293T C258(1.12)  LDD1514  [5]
 LDCM0020  ARS-1620 HCC44 C258(1.43)  LDD0078  [1]
 LDCM0632  CL-Sc Hep-G2 C227(1.56); C268(0.88); C268(0.85); C258(0.57)  LDD2227  [4]
 LDCM0368  CL10 HEK-293T C258(1.44)  LDD1572  [5]
 LDCM0372  CL103 HEK-293T C258(0.92); C227(1.01)  LDD1576  [5]
 LDCM0376  CL107 HEK-293T C258(0.98); C227(0.99)  LDD1580  [5]
 LDCM0381  CL111 HEK-293T C258(1.17); C227(0.97)  LDD1585  [5]
 LDCM0385  CL115 HEK-293T C258(1.46); C227(1.00)  LDD1589  [5]
 LDCM0389  CL119 HEK-293T C258(1.19); C227(1.11)  LDD1593  [5]
 LDCM0390  CL12 HEK-293T C258(1.04)  LDD1594  [5]
 LDCM0394  CL123 HEK-293T C258(0.90); C227(1.01)  LDD1598  [5]
 LDCM0398  CL127 HEK-293T C258(0.90); C227(1.04)  LDD1602  [5]
 LDCM0402  CL15 HEK-293T C258(1.00); C227(1.21)  LDD1606  [5]
 LDCM0404  CL17 HEK-293T C258(1.37)  LDD1608  [5]
 LDCM0406  CL19 HEK-293T C258(0.91)  LDD1610  [5]
 LDCM0408  CL20 HEK-293T C258(0.84)  LDD1612  [5]
 LDCM0409  CL21 HEK-293T C258(1.14)  LDD1613  [5]
 LDCM0410  CL22 HEK-293T C258(0.99)  LDD1614  [5]
 LDCM0412  CL24 HEK-293T C258(1.01)  LDD1616  [5]
 LDCM0415  CL27 HEK-293T C258(1.14); C227(1.05)  LDD1619  [5]
 LDCM0417  CL29 HEK-293T C258(1.41)  LDD1621  [5]
 LDCM0418  CL3 HEK-293T C258(0.96); C227(1.10)  LDD1622  [5]
 LDCM0420  CL31 HEK-293T C258(1.07)  LDD1624  [5]
 LDCM0421  CL32 HEK-293T C258(1.25)  LDD1625  [5]
 LDCM0422  CL33 HEK-293T C258(1.52)  LDD1626  [5]
 LDCM0423  CL34 HEK-293T C258(1.11)  LDD1627  [5]
 LDCM0425  CL36 HEK-293T C258(0.87)  LDD1629  [5]
 LDCM0428  CL39 HEK-293T C258(0.78); C227(0.97)  LDD1632  [5]
 LDCM0431  CL41 HEK-293T C258(1.23)  LDD1635  [5]
 LDCM0433  CL43 HEK-293T C258(0.96)  LDD1637  [5]
 LDCM0434  CL44 HEK-293T C258(0.96)  LDD1638  [5]
 LDCM0435  CL45 HEK-293T C258(1.38)  LDD1639  [5]
 LDCM0436  CL46 HEK-293T C258(0.94)  LDD1640  [5]
 LDCM0438  CL48 HEK-293T C258(1.03)  LDD1642  [5]
 LDCM0440  CL5 HEK-293T C258(0.98)  LDD1644  [5]
 LDCM0444  CL53 HEK-293T C258(1.20)  LDD1647  [5]
 LDCM0446  CL55 HEK-293T C258(1.05)  LDD1649  [5]
 LDCM0447  CL56 HEK-293T C258(1.04)  LDD1650  [5]
 LDCM0448  CL57 HEK-293T C258(1.69)  LDD1651  [5]
 LDCM0449  CL58 HEK-293T C258(0.80)  LDD1652  [5]
 LDCM0452  CL60 HEK-293T C258(1.15)  LDD1655  [5]
 LDCM0455  CL63 HEK-293T C258(1.41); C227(0.99)  LDD1658  [5]
 LDCM0457  CL65 HEK-293T C258(1.14)  LDD1660  [5]
 LDCM0459  CL67 HEK-293T C258(0.96)  LDD1662  [5]
 LDCM0460  CL68 HEK-293T C258(0.95)  LDD1663  [5]
 LDCM0461  CL69 HEK-293T C258(1.51)  LDD1664  [5]
 LDCM0462  CL7 HEK-293T C258(0.86)  LDD1665  [5]
 LDCM0463  CL70 HEK-293T C258(0.86)  LDD1666  [5]
 LDCM0465  CL72 HEK-293T C258(1.07)  LDD1668  [5]
 LDCM0470  CL77 HEK-293T C258(0.93)  LDD1673  [5]
 LDCM0472  CL79 HEK-293T C258(1.21)  LDD1675  [5]
 LDCM0473  CL8 HEK-293T C258(1.66)  LDD1676  [5]
 LDCM0474  CL80 HEK-293T C258(0.87)  LDD1677  [5]
 LDCM0475  CL81 HEK-293T C258(0.88)  LDD1678  [5]
 LDCM0476  CL82 HEK-293T C258(1.00)  LDD1679  [5]
 LDCM0478  CL84 HEK-293T C258(0.99)  LDD1681  [5]
 LDCM0481  CL87 HEK-293T C258(1.10); C227(0.96)  LDD1684  [5]
 LDCM0483  CL89 HEK-293T C258(1.15)  LDD1686  [5]
 LDCM0484  CL9 HEK-293T C258(0.87)  LDD1687  [5]
 LDCM0486  CL91 HEK-293T C258(0.86)  LDD1689  [5]
 LDCM0487  CL92 HEK-293T C258(1.35)  LDD1690  [5]
 LDCM0488  CL93 HEK-293T C258(1.10)  LDD1691  [5]
 LDCM0489  CL94 HEK-293T C258(0.78)  LDD1692  [5]
 LDCM0491  CL96 HEK-293T C258(0.87)  LDD1694  [5]
 LDCM0494  CL99 HEK-293T C258(1.30); C227(0.96)  LDD1697  [5]
 LDCM0495  E2913 HEK-293T C258(0.97); C227(0.95)  LDD1698  [5]
 LDCM0468  Fragment33 HEK-293T C258(1.34); C227(1.09)  LDD1671  [5]
 LDCM0022  KB02 BRX211 C258(2.23)  LDD2268  [6]
 LDCM0023  KB03 BRX390 C258(2.72)  LDD2690  [6]
 LDCM0024  KB05 NCI-H2052 C258(3.76)  LDD3353  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Androgen receptor (AR) Nuclear hormone receptor family P10275

References

1 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
2 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
5 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
6 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