Details of the Target

General Information of Target

Target ID LDTP00012
Target Name Transcription factor E2F8 (E2F8)
Gene Name E2F8
Gene ID 79733
Synonyms
Transcription factor E2F8; E2F-8
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MENEKENLFCEPHKRGLMKTPLKESTTANIVLAEIQPDFGPLTTPTKPKEGSQGEPWTPT
ANLKMLISAVSPEIRNRDQKRGLFDNRSGLPEAKDCIHEHLSGDEFEKSQPSRKEKSLGL
LCHKFLARYPNYPNPAVNNDICLDEVAEELNVERRRIYDIVNVLESLHMVSRLAKNRYTW
HGRHNLNKTLGTLKSIGEENKYAEQIMMIKKKEYEQEFDFIKSYSIEDHIIKSNTGPNGH
PDMCFVELPGVEFRAASVNSRKDKSLRVMSQKFVMLFLVSTPQIVSLEVAAKILIGEDHV
EDLDKSKFKTKIRRLYDIANVLSSLDLIKKVHVTEERGRKPAFKWTGPEISPNTSGSSPV
IHFTPSDLEVRRSSKENCAKNLFSTRGKPNFTRHPSLIKLVKSIESDRRKINSAPSSPIK
TNKAESSQNSAPFPSKMAQLAAICKMQLEEQSSESRQKVKVQLARSGPCKPVAPLDPPVN
AEMELTAPSLIQPLGMVPLIPSPLSSAVPLILPQAPSGPSYAIYLQPTQAHQSVTPPQGL
SPTVCTTHSSKATGSKDSTDATTEKAANDTSKASASTRPGSLLPAPERQGAKSRTREPAG
ERGSKRASMLEDSGSKKKFKEDLKGLENVSATLFPSGYLIPLTQCSSLGAESILSGKENS
SALSPNHRIYSSPIAGVIPVTSSELTAVNFPSFHVTPLKLMVSPTSVAAVPVGNSPALAS
SHPVPIQNPSSAIVNFTLQHLGLISPNVQLSASPGSGIVPVSPRIESVNVAPENAGTQQG
RATNYDSPVPGQSQPNGQSVAVTGAQQPVPVTPKGSQLVAESFFRTPGGPTKPTSSSCMD
FEGANKTSLGTLFVPQRKLEVSTEDVH
Target Bioclass
Transcription factor
Family
E2F/DP family
Subcellular location
Nucleus
Function
Atypical E2F transcription factor that participates in various processes such as angiogenesis and polyploidization of specialized cells. Mainly acts as a transcription repressor that binds DNA independently of DP proteins and specifically recognizes the E2 recognition site 5'-TTTC[CG]CGC-3'. Directly represses transcription of classical E2F transcription factors such as E2F1: component of a feedback loop in S phase by repressing the expression of E2F1, thereby preventing p53/TP53-dependent apoptosis. Plays a key role in polyploidization of cells in placenta and liver by regulating the endocycle, probably by repressing genes promoting cytokinesis and antagonizing action of classical E2F proteins (E2F1, E2F2 and/or E2F3). Required for placental development by promoting polyploidization of trophoblast giant cells. Acts as a promoter of sprouting angiogenesis, possibly by acting as a transcription activator: associates with HIF1A, recognizes and binds the VEGFA promoter, which is different from canonical E2 recognition site, and activates expression of the VEGFA gene.
Uniprot ID
A0AVK6
Ensemble ID
ENST00000250024.9
HGNC ID
HGNC:24727
ChEMBL ID
CHEMBL4630726

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C444(20.00)  LDD1703  [1]
DBIA
 Probe Info  		C96(0.81)  LDD1492  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C122(0.92)  LDD1507  [2]
 LDCM0215  AC10 HEK-293T C444(1.07); C244(1.22); C122(0.95); C645(0.95)  LDD1508  [2]
 LDCM0226  AC11 HEK-293T C244(1.43); C645(0.88)  LDD1509  [2]
 LDCM0270  AC15 HEK-293T C244(1.57); C645(1.17)  LDD1513  [2]
 LDCM0276  AC17 HEK-293T C122(0.97)  LDD1515  [2]
 LDCM0277  AC18 HEK-293T C444(1.05); C244(1.28); C122(0.91); C645(1.13)  LDD1516  [2]
 LDCM0278  AC19 HEK-293T C244(1.93); C645(1.06)  LDD1517  [2]
 LDCM0279  AC2 HEK-293T C444(1.03); C244(0.91); C122(0.98); C645(0.94)  LDD1518  [2]
 LDCM0281  AC21 HEK-293T C444(0.95); C122(1.08); C645(0.79)  LDD1520  [2]
 LDCM0283  AC23 HEK-293T C244(0.97); C645(1.28)  LDD1522  [2]
 LDCM0284  AC24 HEK-293T C244(1.29)  LDD1523  [2]
 LDCM0285  AC25 HEK-293T C122(1.02)  LDD1524  [2]
 LDCM0286  AC26 HEK-293T C444(0.98); C244(1.01); C122(0.93); C645(1.07)  LDD1525  [2]
 LDCM0287  AC27 HEK-293T C244(1.00); C645(1.07)  LDD1526  [2]
 LDCM0289  AC29 HEK-293T C444(1.06); C122(1.01); C645(0.62)  LDD1528  [2]
 LDCM0290  AC3 HEK-293T C244(0.62); C645(0.98)  LDD1529  [2]
 LDCM0292  AC31 HEK-293T C244(1.12); C645(1.08)  LDD1531  [2]
 LDCM0293  AC32 HEK-293T C244(1.10)  LDD1532  [2]
 LDCM0294  AC33 HEK-293T C122(0.94)  LDD1533  [2]
 LDCM0295  AC34 HEK-293T C444(0.99); C244(1.03); C122(1.07); C645(0.95)  LDD1534  [2]
 LDCM0296  AC35 HEK-293T C244(1.44); C645(0.97)  LDD1535  [2]
 LDCM0298  AC37 HEK-293T C444(1.02); C122(0.96); C645(0.73)  LDD1537  [2]
 LDCM0300  AC39 HEK-293T C244(1.37); C645(1.08)  LDD1539  [2]
 LDCM0302  AC40 HEK-293T C244(1.44)  LDD1541  [2]
 LDCM0303  AC41 HEK-293T C122(0.87)  LDD1542  [2]
 LDCM0304  AC42 HEK-293T C444(1.05); C244(1.32); C122(1.03); C645(1.02)  LDD1543  [2]
 LDCM0305  AC43 HEK-293T C244(0.96); C645(0.77)  LDD1544  [2]
 LDCM0307  AC45 HEK-293T C444(1.13); C122(1.06); C645(1.00)  LDD1546  [2]
 LDCM0309  AC47 HEK-293T C244(1.04); C645(1.16)  LDD1548  [2]
 LDCM0310  AC48 HEK-293T C244(0.97)  LDD1549  [2]
 LDCM0311  AC49 HEK-293T C122(0.95)  LDD1550  [2]
 LDCM0312  AC5 HEK-293T C444(0.94); C122(1.01); C645(0.70)  LDD1551  [2]
 LDCM0313  AC50 HEK-293T C444(1.05); C244(1.50); C122(1.06); C645(1.03)  LDD1552  [2]
 LDCM0314  AC51 HEK-293T C244(1.01); C645(1.07)  LDD1553  [2]
 LDCM0316  AC53 HEK-293T C444(0.97); C122(1.03); C645(0.71)  LDD1555  [2]
 LDCM0318  AC55 HEK-293T C244(1.18); C645(1.10)  LDD1557  [2]
 LDCM0319  AC56 HEK-293T C244(1.05)  LDD1558  [2]
 LDCM0320  AC57 HEK-293T C122(0.95)  LDD1559  [2]
 LDCM0321  AC58 HEK-293T C444(1.07); C244(1.40); C122(0.95); C645(1.08)  LDD1560  [2]
 LDCM0322  AC59 HEK-293T C244(0.70); C645(1.07)  LDD1561  [2]
 LDCM0325  AC61 HEK-293T C444(0.98); C122(0.99); C645(0.77)  LDD1564  [2]
 LDCM0327  AC63 HEK-293T C244(1.20); C645(1.10)  LDD1566  [2]
 LDCM0328  AC64 HEK-293T C244(1.17)  LDD1567  [2]
 LDCM0334  AC7 HEK-293T C244(1.01); C645(1.09)  LDD1568  [2]
 LDCM0345  AC8 HEK-293T C244(1.33)  LDD1569  [2]
 LDCM0248  AKOS034007472 HEK-293T C444(1.09); C122(1.01); C645(0.66)  LDD1511  [2]
 LDCM0356  AKOS034007680 HEK-293T C122(0.91)  LDD1570  [2]
 LDCM0275  AKOS034007705 HEK-293T C244(1.34)  LDD1514  [2]
 LDCM0367  CL1 HEK-293T C444(1.09)  LDD1571  [2]
 LDCM0369  CL100 HEK-293T C444(0.98); C122(0.98); C645(1.13)  LDD1573  [2]
 LDCM0370  CL101 HEK-293T C444(1.05)  LDD1574  [2]
 LDCM0371  CL102 HEK-293T C122(0.94); C645(1.28)  LDD1575  [2]
 LDCM0372  CL103 HEK-293T C122(1.01)  LDD1576  [2]
 LDCM0373  CL104 HEK-293T C444(1.03); C122(1.00); C645(1.12)  LDD1577  [2]
 LDCM0374  CL105 HEK-293T C444(1.05)  LDD1578  [2]
 LDCM0375  CL106 HEK-293T C122(1.00); C645(1.05)  LDD1579  [2]
 LDCM0376  CL107 HEK-293T C122(1.12)  LDD1580  [2]
 LDCM0377  CL108 HEK-293T C444(0.94); C122(0.98); C645(1.23)  LDD1581  [2]
 LDCM0378  CL109 HEK-293T C444(0.96)  LDD1582  [2]
 LDCM0379  CL11 HEK-293T C244(1.32); C645(1.03)  LDD1583  [2]
 LDCM0380  CL110 HEK-293T C122(0.97); C645(0.81)  LDD1584  [2]
 LDCM0381  CL111 HEK-293T C122(0.97)  LDD1585  [2]
 LDCM0382  CL112 HEK-293T C444(0.96); C122(0.90); C645(1.13)  LDD1586  [2]
 LDCM0383  CL113 HEK-293T C444(1.10)  LDD1587  [2]
 LDCM0384  CL114 HEK-293T C122(1.04); C645(0.96)  LDD1588  [2]
 LDCM0385  CL115 HEK-293T C122(1.01)  LDD1589  [2]
 LDCM0386  CL116 HEK-293T C444(1.01); C122(0.99); C645(1.16)  LDD1590  [2]
 LDCM0387  CL117 HEK-293T C444(1.13)  LDD1591  [2]
 LDCM0388  CL118 HEK-293T C122(1.05); C645(1.07)  LDD1592  [2]
 LDCM0389  CL119 HEK-293T C122(1.07)  LDD1593  [2]
 LDCM0390  CL12 HEK-293T C244(1.04)  LDD1594  [2]
 LDCM0391  CL120 HEK-293T C444(1.07); C122(1.06); C645(1.17)  LDD1595  [2]
 LDCM0392  CL121 HEK-293T C444(1.09)  LDD1596  [2]
 LDCM0393  CL122 HEK-293T C122(0.97); C645(0.94)  LDD1597  [2]
 LDCM0394  CL123 HEK-293T C122(0.91)  LDD1598  [2]
 LDCM0395  CL124 HEK-293T C444(1.06); C122(0.98); C645(1.14)  LDD1599  [2]
 LDCM0396  CL125 HEK-293T C444(1.03)  LDD1600  [2]
 LDCM0397  CL126 HEK-293T C122(1.00); C645(0.83)  LDD1601  [2]
 LDCM0398  CL127 HEK-293T C122(0.95)  LDD1602  [2]
 LDCM0399  CL128 HEK-293T C444(1.01); C122(1.01); C645(1.03)  LDD1603  [2]
 LDCM0400  CL13 HEK-293T C444(1.18)  LDD1604  [2]
 LDCM0401  CL14 HEK-293T C122(0.98); C645(0.98)  LDD1605  [2]
 LDCM0402  CL15 HEK-293T C122(0.95)  LDD1606  [2]
 LDCM0403  CL16 HEK-293T C444(0.98); C122(1.04); C645(1.28)  LDD1607  [2]
 LDCM0404  CL17 HEK-293T C122(0.79)  LDD1608  [2]
 LDCM0405  CL18 HEK-293T C444(1.02); C244(1.12); C122(0.99); C645(0.91)  LDD1609  [2]
 LDCM0406  CL19 HEK-293T C244(0.80); C645(1.01)  LDD1610  [2]
 LDCM0407  CL2 HEK-293T C122(1.02); C645(0.88)  LDD1611  [2]
 LDCM0409  CL21 HEK-293T C444(0.99); C122(0.92); C645(0.85)  LDD1613  [2]
 LDCM0411  CL23 HEK-293T C244(1.01); C645(1.16)  LDD1615  [2]
 LDCM0412  CL24 HEK-293T C244(1.26)  LDD1616  [2]
 LDCM0413  CL25 HEK-293T C444(1.09)  LDD1617  [2]
 LDCM0414  CL26 HEK-293T C122(0.97); C645(0.86)  LDD1618  [2]
 LDCM0415  CL27 HEK-293T C122(1.07)  LDD1619  [2]
 LDCM0416  CL28 HEK-293T C444(0.91); C122(1.01); C645(0.97)  LDD1620  [2]
 LDCM0417  CL29 HEK-293T C122(0.95)  LDD1621  [2]
 LDCM0418  CL3 HEK-293T C122(0.94)  LDD1622  [2]
 LDCM0419  CL30 HEK-293T C444(1.00); C244(1.23); C122(1.03); C645(0.90)  LDD1623  [2]
 LDCM0420  CL31 HEK-293T C244(0.69); C645(0.76)  LDD1624  [2]
 LDCM0422  CL33 HEK-293T C444(1.04); C122(1.16); C645(0.51)  LDD1626  [2]
 LDCM0424  CL35 HEK-293T C244(0.84); C645(1.16)  LDD1628  [2]
 LDCM0425  CL36 HEK-293T C244(0.88)  LDD1629  [2]
 LDCM0426  CL37 HEK-293T C444(1.12)  LDD1630  [2]
 LDCM0428  CL39 HEK-293T C122(0.91)  LDD1632  [2]
 LDCM0429  CL4 HEK-293T C444(0.96); C122(1.11); C645(1.23)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C444(1.00); C122(1.00); C645(1.11)  LDD1634  [2]
 LDCM0431  CL41 HEK-293T C122(1.05)  LDD1635  [2]
 LDCM0432  CL42 HEK-293T C444(1.01); C244(1.10); C122(0.96); C645(0.95)  LDD1636  [2]
 LDCM0433  CL43 HEK-293T C244(0.95); C645(0.70)  LDD1637  [2]
 LDCM0435  CL45 HEK-293T C444(0.94); C122(0.86); C645(0.86)  LDD1639  [2]
 LDCM0437  CL47 HEK-293T C244(1.16); C645(1.21)  LDD1641  [2]
 LDCM0438  CL48 HEK-293T C244(0.81)  LDD1642  [2]
 LDCM0439  CL49 HEK-293T C444(1.12)  LDD1643  [2]
 LDCM0440  CL5 HEK-293T C122(0.88)  LDD1644  [2]
 LDCM0441  CL50 HEK-293T C122(1.05); C645(0.82)  LDD1645  [2]
 LDCM0443  CL52 HEK-293T C444(1.04); C122(1.03); C645(1.15)  LDD1646  [2]
 LDCM0444  CL53 HEK-293T C122(0.85)  LDD1647  [2]
 LDCM0445  CL54 HEK-293T C444(1.04); C244(1.24); C122(0.87); C645(0.87)  LDD1648  [2]
 LDCM0446  CL55 HEK-293T C244(0.62); C645(0.99)  LDD1649  [2]
 LDCM0448  CL57 HEK-293T C444(1.05); C122(0.99); C645(0.92)  LDD1651  [2]
 LDCM0450  CL59 HEK-293T C244(0.98); C645(1.14)  LDD1653  [2]
 LDCM0451  CL6 HEK-293T C444(1.14); C244(1.27); C122(1.13); C645(0.89)  LDD1654  [2]
 LDCM0452  CL60 HEK-293T C244(1.15)  LDD1655  [2]
 LDCM0453  CL61 HEK-293T C444(1.12)  LDD1656  [2]
 LDCM0454  CL62 HEK-293T C122(1.11); C645(1.33)  LDD1657  [2]
 LDCM0455  CL63 HEK-293T C122(1.06)  LDD1658  [2]
 LDCM0456  CL64 HEK-293T C444(1.00); C122(0.94); C645(0.85)  LDD1659  [2]
 LDCM0457  CL65 HEK-293T C122(0.93)  LDD1660  [2]
 LDCM0458  CL66 HEK-293T C444(1.10); C244(1.18); C122(0.86); C645(0.94)  LDD1661  [2]
 LDCM0459  CL67 HEK-293T C244(0.81); C645(1.18)  LDD1662  [2]
 LDCM0461  CL69 HEK-293T C444(0.99); C122(1.11); C645(0.70)  LDD1664  [2]
 LDCM0462  CL7 HEK-293T C244(1.02); C645(0.91)  LDD1665  [2]
 LDCM0464  CL71 HEK-293T C244(0.95); C645(1.13)  LDD1667  [2]
 LDCM0465  CL72 HEK-293T C244(1.20)  LDD1668  [2]
 LDCM0466  CL73 HEK-293T C444(1.07)  LDD1669  [2]
 LDCM0467  CL74 HEK-293T C122(1.02); C645(1.00)  LDD1670  [2]
 LDCM0469  CL76 HEK-293T C444(0.98); C122(1.07); C645(1.22)  LDD1672  [2]
 LDCM0470  CL77 HEK-293T C122(0.90)  LDD1673  [2]
 LDCM0471  CL78 HEK-293T C444(0.99); C244(1.35); C122(0.96); C645(1.02)  LDD1674  [2]
 LDCM0472  CL79 HEK-293T C244(1.06); C645(0.85)  LDD1675  [2]
 LDCM0475  CL81 HEK-293T C444(1.09); C122(1.03); C645(0.65)  LDD1678  [2]
 LDCM0477  CL83 HEK-293T C244(1.30); C645(0.93)  LDD1680  [2]
 LDCM0478  CL84 HEK-293T C244(1.04)  LDD1681  [2]
 LDCM0479  CL85 HEK-293T C444(1.07)  LDD1682  [2]
 LDCM0480  CL86 HEK-293T C122(1.03); C645(0.92)  LDD1683  [2]
 LDCM0481  CL87 HEK-293T C122(1.04)  LDD1684  [2]
 LDCM0482  CL88 HEK-293T C444(1.13); C122(1.00); C645(1.17)  LDD1685  [2]
 LDCM0483  CL89 HEK-293T C122(0.85)  LDD1686  [2]
 LDCM0484  CL9 HEK-293T C444(1.02); C122(1.08); C645(0.64)  LDD1687  [2]
 LDCM0485  CL90 HEK-293T C444(1.03); C244(1.40); C122(0.32); C645(1.01)  LDD1688  [2]
 LDCM0486  CL91 HEK-293T C244(0.56); C645(0.73)  LDD1689  [2]
 LDCM0488  CL93 HEK-293T C444(1.11); C122(0.94); C645(0.47)  LDD1691  [2]
 LDCM0490  CL95 HEK-293T C244(1.24); C645(1.26)  LDD1693  [2]
 LDCM0491  CL96 HEK-293T C244(0.88)  LDD1694  [2]
 LDCM0492  CL97 HEK-293T C444(1.05)  LDD1695  [2]
 LDCM0493  CL98 HEK-293T C122(1.00); C645(0.91)  LDD1696  [2]
 LDCM0494  CL99 HEK-293T C122(0.92)  LDD1697  [2]
 LDCM0495  E2913 HEK-293T C122(0.94)  LDD1698  [2]
 LDCM0468  Fragment33 HEK-293T C122(0.98)  LDD1671  [2]
 LDCM0427  Fragment51 HEK-293T C122(1.18); C645(1.02)  LDD1631  [2]
 LDCM0022  KB02 HEK-293T C96(0.81)  LDD1492  [2]
 LDCM0023  KB03 HEK-293T C96(1.02)  LDD1497  [2]
 LDCM0024  KB05 HEK-293T C96(0.88)  LDD1502  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Caspase-6 (CASP6) Peptidase C14A family P55212
Fibroblast growth factor receptor 3 (FGFR3) Tyr protein kinase family P22607
GTPase HRas (HRAS) Ras family P01112
E3 ubiquitin-protein ligase CHIP (STUB1) . Q9UNE7
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Glutamate receptor ionotropic, NMDA 2C (GRIN2C) Glutamate-gated ion channel family Q14957
Huntingtin (HTT) Huntingtin family P42858
Peroxisome assembly protein 26 (PEX26) Peroxin-26 family Q7Z412
Alpha-synuclein (SNCA) Synuclein family P37840
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor E2F7 (E2F7) E2F/DP family Q96AV8
Alpha-globin transcription factor CP2 (TFCP2) Grh/CP2 family Q12800
Krueppel-like factor 11 (KLF11) Sp1 C2H2-type zinc-finger protein family O14901
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Beta-2 adrenergic receptor (ADRB2) G-protein coupled receptor 1 family P07550
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Axonemal dynein light intermediate polypeptide 1 (DNALI1) Inner dynein arm light chain family O14645
Gelsolin (GSN) Villin/gelsolin family P06396
Four and a half LIM domains protein 3 (FHL3) . Q13643
Ubiquilin-1 (UBQLN1) . Q9UMX0

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.
2 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