General Information of Target

Target ID LDTP02156
Target Name Eukaryotic translation initiation factor 4E (EIF4E)
Gene Name EIF4E
Gene ID 1977
Synonyms
EIF4EL1; EIF4F; Eukaryotic translation initiation factor 4E; eIF-4E; eIF4E; eIF-4F 25 kDa subunit; mRNA cap-binding protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATVEPETTPTPNPPTTEEEKTESNQEVANPEHYIKHPLQNRWALWFFKNDKSKTWQANL
RLISKFDTVEDFWALYNHIQLSSNLMPGCDYSLFKDGIEPMWEDEKNKRGGRWLITLNKQ
QRRSDLDRFWLETLLCLIGESFDDYSDDVCGAVVNVRAKGDKIAIWTTECENREAVTHIG
RVYKERLGLPPKIVIGYQSHADTATKSGSTTKNRFVV
Target Type
Literature-reported
Target Bioclass
Other
Family
Eukaryotic initiation factor 4E family
Subcellular location
Cytoplasm, P-body
Function
Acts in the cytoplasm to initiate and regulate protein synthesis and is required in the nucleus for export of a subset of mRNAs from the nucleus to the cytoplasm which promotes processes such as RNA capping, processing and splicing. Component of the protein complex eIF4F, which is involved in the recognition of the mRNA cap, ATP-dependent unwinding of 5'-terminal secondary structure and recruitment of mRNA to the ribosome. This protein recognizes and binds the 7-methylguanosine (m7G)-containing mRNA cap during an early step in the initiation of protein synthesis and facilitates ribosome binding by inducing the unwinding of the mRNAs secondary structures. Together with EIF4G1, antagonizes the scanning promoted by EIF1-EIF4G1 and is required for TISU translation, a process where the TISU element recognition makes scanning unnecessary. In addition to its role in translation initiation, also acts as a regulator of translation and stability in the cytoplasm. Component of the CYFIP1-EIF4E-FMR1 complex which binds to the mRNA cap and mediates translational repression: in the complex, EIF4E mediates the binding to the mRNA cap. Component of a multiprotein complex that sequesters and represses translation of proneurogenic factors during neurogenesis. In P-bodies, component of a complex that mediates the storage of translationally inactive mRNAs in the cytoplasm and prevents their degradation. May play an important role in spermatogenesis through translational regulation of stage-specific mRNAs during germ cell development. As well as its roles in translation, also involved in mRNA nucleocytoplasmic transport. Its role in mRNA export from the nucleus to the cytoplasm relies on its ability to bind the m7G cap of RNAs and on the presence of the 50-nucleotide EIF4E sensitivity element (4ESE) in the 3'UTR of sensitive transcripts. Interaction with the 4ESE is mediated by LRPPRC which binds simultaneously to both EIF4E and the 4ESE, thereby acting as a platform for assembly for the RNA export complex. EIF4E-dependent mRNA export is independent of ongoing protein or RNA synthesis and is also NFX1-independent but is XPO1-dependent with LRPPRC interacting with XPO1 to form an EIF4E-dependent mRNA export complex. Alters the composition of the cytoplasmic face of the nuclear pore to promote RNA export by reducing RANBP2 expression, relocalizing nucleoporin NUP214 and increasing expression of RANBP1 and RNA export factors DDX19 and GLE1. Promotes the nuclear export of cyclin CCND1 mRNA. Promotes the nuclear export of NOS2/iNOS mRNA. Promotes the nuclear export of MDM2 mRNA. Promotes the export of additional mRNAs, including others involved in the cell cycle. In the nucleus, binds to capped splice factor-encoding mRNAs and stimulates their nuclear export to enhance splice factor production by increasing their cytoplasmic availability to the translation machinery. May also regulate splicing through interaction with the spliceosome in an RNA and m7G cap-dependent manner. Also binds to some pre-mRNAs and may play a role in their recruitment to the spliceosome. Promotes steady-state capping of a subset of coding and non-coding RNAs by mediating nuclear export of capping machinery mRNAs including RNMT, RNGTT and RAMAC to enhance their translation. Stimulates mRNA 3'-end processing by promoting the expression of several core cleavage complex factors required for mRNA cleavage and polyadenylation, and may also have a direct effect through its interaction with the CPSF3 cleavage enzyme. Rescues cells from apoptosis by promoting activation of serine/threonine-protein kinase AKT1 through mRNA export of NBS1 which potentiates AKT1 phosphorylation and also through mRNA export of AKT1 effectors, allowing for increased production of these proteins.
TTD ID
T48614
Uniprot ID
P06730
DrugMap ID
TTUF10B
Ensemble ID
ENST00000280892.10
HGNC ID
HGNC:3287
ChEMBL ID
CHEMBL4848

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.L114P DBIA    Probe Info 
DU145 SNV: p.P12H DBIA    Probe Info 
HCT15 SNV: p.A74V DBIA    Probe Info 
MFE319 SNV: p.A44T DBIA    Probe Info 
SW403 SNV: p.E19Ter DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 32 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
11.57  LDD0402  [1]
TH211
 Probe Info 
Y197(9.39)  LDD0260  [2]
ONAyne
 Probe Info 
K212(5.00)  LDD0274  [3]
IPM
 Probe Info 
N.A.  LDD0241  [4]
Probe 1
 Probe Info 
Y34(18.58); Y197(24.08)  LDD3495  [5]
DBIA
 Probe Info 
C201(1.55)  LDD3310  [6]
BTD
 Probe Info 
C170(1.08)  LDD2125  [7]
HHS-475
 Probe Info 
Y34(1.01)  LDD0264  [8]
HHS-465
 Probe Info 
Y34(10.00)  LDD2237  [9]
5E-2FA
 Probe Info 
H178(0.00); H200(0.00); H33(0.00)  LDD2235  [10]
ATP probe
 Probe Info 
K206(0.00); K159(0.00); K162(0.00); K119(0.00)  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info 
C89(0.00); C170(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [13]
IPIAA_H
 Probe Info 
N.A.  LDD0030  [14]
IPIAA_L
 Probe Info 
N.A.  LDD0031  [14]
Lodoacetamide azide
 Probe Info 
C89(0.00); C170(0.00)  LDD0037  [12]
ATP probe
 Probe Info 
K49(0.00); K162(0.00)  LDD0035  [15]
NAIA_4
 Probe Info 
C136(0.00); C170(0.00)  LDD2226  [16]
WYneN
 Probe Info 
N.A.  LDD0021  [17]
Compound 10
 Probe Info 
N.A.  LDD2216  [18]
NHS
 Probe Info 
K119(0.00); K206(0.00)  LDD0010  [17]
OSF
 Probe Info 
N.A.  LDD0029  [19]
SF
 Probe Info 
N.A.  LDD0028  [19]
STPyne
 Probe Info 
N.A.  LDD0009  [17]
Ox-W18
 Probe Info 
W113(0.00); W166(0.00)  LDD2175  [20]
1c-yne
 Probe Info 
N.A.  LDD0228  [21]
Acrolein
 Probe Info 
C170(0.00); H200(0.00)  LDD0217  [22]
Cinnamaldehyde
 Probe Info 
N.A.  LDD0220  [22]
Crotonaldehyde
 Probe Info 
N.A.  LDD0219  [22]
Methacrolein
 Probe Info 
N.A.  LDD0218  [22]
AOyne
 Probe Info 
7.80  LDD0443  [23]
NAIA_5
 Probe Info 
N.A.  LDD2223  [16]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C219
 Probe Info 
11.39  LDD1893  [24]
C260
 Probe Info 
5.66  LDD1932  [24]
FFF probe14
 Probe Info 
5.26  LDD0477  [25]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C170(0.94); C89(1.04)  LDD1507  [26]
 LDCM0215  AC10 HEK-293T C170(0.81); C89(1.12)  LDD1508  [26]
 LDCM0226  AC11 HEK-293T C170(0.92); C89(0.99)  LDD1509  [26]
 LDCM0237  AC12 HEK-293T C170(0.92); C89(1.00); C136(1.06)  LDD1510  [26]
 LDCM0259  AC14 HEK-293T C170(1.06); C89(0.95)  LDD1512  [26]
 LDCM0270  AC15 HEK-293T C170(0.92); C89(1.10)  LDD1513  [26]
 LDCM0276  AC17 HEK-293T C170(0.97); C89(1.08)  LDD1515  [26]
 LDCM0277  AC18 HEK-293T C170(0.96); C89(0.92)  LDD1516  [26]
 LDCM0278  AC19 HEK-293T C170(0.88); C89(0.96)  LDD1517  [26]
 LDCM0279  AC2 HEK-293T C170(0.91); C89(0.97)  LDD1518  [26]
 LDCM0280  AC20 HEK-293T C170(1.04); C89(1.00); C136(1.14)  LDD1519  [26]
 LDCM0281  AC21 HEK-293T C170(0.97); C89(0.91)  LDD1520  [26]
 LDCM0282  AC22 HEK-293T C170(1.02); C89(0.92)  LDD1521  [26]
 LDCM0283  AC23 HEK-293T C170(1.06); C89(1.02)  LDD1522  [26]
 LDCM0284  AC24 HEK-293T C170(1.01); C89(1.06)  LDD1523  [26]
 LDCM0285  AC25 HEK-293T C170(0.97); C89(1.05)  LDD1524  [26]
 LDCM0286  AC26 HEK-293T C170(0.94); C89(1.03)  LDD1525  [26]
 LDCM0287  AC27 HEK-293T C170(0.93); C89(0.89)  LDD1526  [26]
 LDCM0288  AC28 HEK-293T C170(0.96); C89(1.04); C136(1.28)  LDD1527  [26]
 LDCM0289  AC29 HEK-293T C170(0.98); C89(0.90)  LDD1528  [26]
 LDCM0290  AC3 HEK-293T C170(0.83); C89(0.98)  LDD1529  [26]
 LDCM0291  AC30 HEK-293T C170(0.98); C89(0.87)  LDD1530  [26]
 LDCM0292  AC31 HEK-293T C170(0.95); C89(1.03)  LDD1531  [26]
 LDCM0293  AC32 HEK-293T C170(1.02); C89(1.08)  LDD1532  [26]
 LDCM0294  AC33 HEK-293T C170(0.91); C89(1.10)  LDD1533  [26]
 LDCM0295  AC34 HEK-293T C170(0.99); C89(0.94)  LDD1534  [26]
 LDCM0296  AC35 HEK-293T C170(0.91); C89(0.99)  LDD1535  [26]
 LDCM0297  AC36 HEK-293T C170(0.97); C89(0.99); C136(0.90)  LDD1536  [26]
 LDCM0298  AC37 HEK-293T C170(1.06); C89(0.91)  LDD1537  [26]
 LDCM0299  AC38 HEK-293T C170(1.01); C89(0.88)  LDD1538  [26]
 LDCM0300  AC39 HEK-293T C170(1.00); C89(1.17)  LDD1539  [26]
 LDCM0301  AC4 HEK-293T C170(0.99); C89(1.00); C136(1.06)  LDD1540  [26]
 LDCM0302  AC40 HEK-293T C170(0.98); C89(0.94)  LDD1541  [26]
 LDCM0303  AC41 HEK-293T C170(0.96); C89(1.15)  LDD1542  [26]
 LDCM0304  AC42 HEK-293T C170(1.00); C89(1.00)  LDD1543  [26]
 LDCM0305  AC43 HEK-293T C170(0.84); C89(0.96)  LDD1544  [26]
 LDCM0306  AC44 HEK-293T C170(0.99); C89(1.09); C136(1.14)  LDD1545  [26]
 LDCM0307  AC45 HEK-293T C170(0.90); C89(1.03)  LDD1546  [26]
 LDCM0308  AC46 HEK-293T C170(1.00); C89(0.84)  LDD1547  [26]
 LDCM0309  AC47 HEK-293T C170(1.02); C89(1.00)  LDD1548  [26]
 LDCM0310  AC48 HEK-293T C170(1.00); C89(1.05)  LDD1549  [26]
 LDCM0311  AC49 HEK-293T C170(0.89); C89(1.07)  LDD1550  [26]
 LDCM0312  AC5 HEK-293T C170(0.93); C89(1.04)  LDD1551  [26]
 LDCM0313  AC50 HEK-293T C170(0.90); C89(0.99)  LDD1552  [26]
 LDCM0314  AC51 HEK-293T C170(0.89); C89(1.02)  LDD1553  [26]
 LDCM0315  AC52 HEK-293T C170(0.90); C89(0.97); C136(0.91)  LDD1554  [26]
 LDCM0316  AC53 HEK-293T C170(0.92); C89(0.96)  LDD1555  [26]
 LDCM0317  AC54 HEK-293T C170(0.99); C89(0.95)  LDD1556  [26]
 LDCM0318  AC55 HEK-293T C170(0.96); C89(1.09)  LDD1557  [26]
 LDCM0319  AC56 HEK-293T C170(1.04); C89(1.01)  LDD1558  [26]
 LDCM0320  AC57 HEK-293T C170(0.90); C89(1.11)  LDD1559  [26]
 LDCM0321  AC58 HEK-293T C170(0.90); C89(1.04)  LDD1560  [26]
 LDCM0322  AC59 HEK-293T C170(0.95); C89(0.99)  LDD1561  [26]
 LDCM0323  AC6 HEK-293T C170(0.87); C89(0.90)  LDD1562  [26]
 LDCM0324  AC60 HEK-293T C170(0.90); C89(1.00); C136(1.16)  LDD1563  [26]
 LDCM0325  AC61 HEK-293T C170(0.94); C89(1.01)  LDD1564  [26]
 LDCM0326  AC62 HEK-293T C170(1.05); C89(0.86)  LDD1565  [26]
 LDCM0327  AC63 HEK-293T C170(1.01); C89(0.95)  LDD1566  [26]
 LDCM0328  AC64 HEK-293T C170(1.00); C89(0.96)  LDD1567  [26]
 LDCM0334  AC7 HEK-293T C170(0.92); C89(0.97)  LDD1568  [26]
 LDCM0345  AC8 HEK-293T C170(0.99); C89(0.99)  LDD1569  [26]
 LDCM0248  AKOS034007472 HEK-293T C170(0.94); C89(1.10)  LDD1511  [26]
 LDCM0356  AKOS034007680 HEK-293T C170(0.87); C89(1.00)  LDD1570  [26]
 LDCM0275  AKOS034007705 HEK-293T C170(0.95); C89(1.04)  LDD1514  [26]
 LDCM0156  Aniline NCI-H1299 12.12  LDD0403  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [22]
 LDCM0632  CL-Sc Hep-G2 C170(1.45)  LDD2227  [16]
 LDCM0367  CL1 HEK-293T C170(0.89); C89(1.06)  LDD1571  [26]
 LDCM0368  CL10 HEK-293T C170(1.15); C89(1.13)  LDD1572  [26]
 LDCM0369  CL100 HEK-293T C170(1.00); C89(1.03)  LDD1573  [26]
 LDCM0370  CL101 HEK-293T C170(0.96); C89(0.99)  LDD1574  [26]
 LDCM0371  CL102 HEK-293T C170(0.96); C89(1.01)  LDD1575  [26]
 LDCM0372  CL103 HEK-293T C170(0.87); C89(0.94)  LDD1576  [26]
 LDCM0373  CL104 HEK-293T C170(0.95); C89(1.12)  LDD1577  [26]
 LDCM0374  CL105 HEK-293T C170(0.94); C89(1.00)  LDD1578  [26]
 LDCM0375  CL106 HEK-293T C170(1.00); C89(0.90)  LDD1579  [26]
 LDCM0376  CL107 HEK-293T C170(0.94); C89(1.03)  LDD1580  [26]
 LDCM0377  CL108 HEK-293T C170(1.00); C89(1.03)  LDD1581  [26]
 LDCM0378  CL109 HEK-293T C170(0.91); C89(1.05)  LDD1582  [26]
 LDCM0379  CL11 HEK-293T C170(1.00); C89(1.19)  LDD1583  [26]
 LDCM0380  CL110 HEK-293T C170(0.98); C89(0.87)  LDD1584  [26]
 LDCM0381  CL111 HEK-293T C170(0.91); C89(0.95)  LDD1585  [26]
 LDCM0382  CL112 HEK-293T C170(0.98); C89(1.18)  LDD1586  [26]
 LDCM0383  CL113 HEK-293T C170(0.94); C89(0.97)  LDD1587  [26]
 LDCM0384  CL114 HEK-293T C170(0.92); C89(0.94)  LDD1588  [26]
 LDCM0385  CL115 HEK-293T C170(0.92); C89(0.85)  LDD1589  [26]
 LDCM0386  CL116 HEK-293T C170(0.97); C89(1.06)  LDD1590  [26]
 LDCM0387  CL117 HEK-293T C170(0.99); C89(1.06)  LDD1591  [26]
 LDCM0388  CL118 HEK-293T C170(0.95); C89(0.89)  LDD1592  [26]
 LDCM0389  CL119 HEK-293T C170(0.97); C89(0.98)  LDD1593  [26]
 LDCM0390  CL12 HEK-293T C170(0.94); C89(1.05)  LDD1594  [26]
 LDCM0391  CL120 HEK-293T C170(0.87); C89(1.10)  LDD1595  [26]
 LDCM0392  CL121 HEK-293T C170(0.93); C89(1.03)  LDD1596  [26]
 LDCM0393  CL122 HEK-293T C170(0.96); C89(1.01)  LDD1597  [26]
 LDCM0394  CL123 HEK-293T C170(1.00); C89(0.95)  LDD1598  [26]
 LDCM0395  CL124 HEK-293T C170(0.93); C89(1.18)  LDD1599  [26]
 LDCM0396  CL125 HEK-293T C170(0.96); C89(1.05)  LDD1600  [26]
 LDCM0397  CL126 HEK-293T C170(0.93); C89(0.97)  LDD1601  [26]
 LDCM0398  CL127 HEK-293T C170(0.86); C89(0.89)  LDD1602  [26]
 LDCM0399  CL128 HEK-293T C170(0.95); C89(0.99)  LDD1603  [26]
 LDCM0400  CL13 HEK-293T C170(0.91); C89(1.12)  LDD1604  [26]
 LDCM0401  CL14 HEK-293T C170(0.97); C89(0.81)  LDD1605  [26]
 LDCM0402  CL15 HEK-293T C170(0.92); C89(1.12)  LDD1606  [26]
 LDCM0403  CL16 HEK-293T C170(0.95); C89(0.91)  LDD1607  [26]
 LDCM0404  CL17 HEK-293T C170(0.87); C89(1.18)  LDD1608  [26]
 LDCM0405  CL18 HEK-293T C170(0.89); C89(0.96)  LDD1609  [26]
 LDCM0406  CL19 HEK-293T C170(0.90); C89(1.07)  LDD1610  [26]
 LDCM0407  CL2 HEK-293T C170(0.91); C89(0.73)  LDD1611  [26]
 LDCM0408  CL20 HEK-293T C170(1.07); C89(1.08); C136(0.95)  LDD1612  [26]
 LDCM0409  CL21 HEK-293T C170(0.90); C89(1.19)  LDD1613  [26]
 LDCM0410  CL22 HEK-293T C170(1.07); C89(1.17)  LDD1614  [26]
 LDCM0411  CL23 HEK-293T C170(1.00); C89(1.07)  LDD1615  [26]
 LDCM0412  CL24 HEK-293T C170(1.15); C89(1.01)  LDD1616  [26]
 LDCM0413  CL25 HEK-293T C170(0.97); C89(0.97)  LDD1617  [26]
 LDCM0414  CL26 HEK-293T C170(1.01); C89(0.96)  LDD1618  [26]
 LDCM0415  CL27 HEK-293T C170(0.95); C89(1.05)  LDD1619  [26]
 LDCM0416  CL28 HEK-293T C170(0.95); C89(1.15)  LDD1620  [26]
 LDCM0417  CL29 HEK-293T C170(0.98); C89(1.01)  LDD1621  [26]
 LDCM0418  CL3 HEK-293T C170(0.93); C89(1.03)  LDD1622  [26]
 LDCM0419  CL30 HEK-293T C170(0.92); C89(0.93)  LDD1623  [26]
 LDCM0420  CL31 HEK-293T C170(0.85); C89(0.96)  LDD1624  [26]
 LDCM0421  CL32 HEK-293T C170(0.96); C89(0.97); C136(1.07)  LDD1625  [26]
 LDCM0422  CL33 HEK-293T C170(1.02); C89(1.23)  LDD1626  [26]
 LDCM0423  CL34 HEK-293T C170(1.07); C89(0.86)  LDD1627  [26]
 LDCM0424  CL35 HEK-293T C170(1.04); C89(1.05)  LDD1628  [26]
 LDCM0425  CL36 HEK-293T C170(1.12); C89(1.01)  LDD1629  [26]
 LDCM0426  CL37 HEK-293T C170(0.98); C89(1.19)  LDD1630  [26]
 LDCM0428  CL39 HEK-293T C170(0.88); C89(1.07)  LDD1632  [26]
 LDCM0429  CL4 HEK-293T C170(0.98); C89(0.96)  LDD1633  [26]
 LDCM0430  CL40 HEK-293T C170(0.93); C89(1.09)  LDD1634  [26]
 LDCM0431  CL41 HEK-293T C170(0.96); C89(1.24)  LDD1635  [26]
 LDCM0432  CL42 HEK-293T C170(0.88); C89(0.93)  LDD1636  [26]
 LDCM0433  CL43 HEK-293T C170(0.92); C89(0.94)  LDD1637  [26]
 LDCM0434  CL44 HEK-293T C170(1.05); C89(0.99); C136(0.82)  LDD1638  [26]
 LDCM0435  CL45 HEK-293T C170(0.98); C89(1.18)  LDD1639  [26]
 LDCM0436  CL46 HEK-293T C170(1.11); C89(0.90)  LDD1640  [26]
 LDCM0437  CL47 HEK-293T C170(1.05); C89(1.00)  LDD1641  [26]
 LDCM0438  CL48 HEK-293T C170(0.99); C89(0.99)  LDD1642  [26]
 LDCM0439  CL49 HEK-293T C170(1.04); C89(1.20)  LDD1643  [26]
 LDCM0440  CL5 HEK-293T C170(0.95); C89(1.25)  LDD1644  [26]
 LDCM0441  CL50 HEK-293T C170(0.97); C89(0.85)  LDD1645  [26]
 LDCM0443  CL52 HEK-293T C170(0.91); C89(1.04)  LDD1646  [26]
 LDCM0444  CL53 HEK-293T C170(0.89); C89(1.33)  LDD1647  [26]
 LDCM0445  CL54 HEK-293T C170(0.82); C89(1.18)  LDD1648  [26]
 LDCM0446  CL55 HEK-293T C170(0.93); C89(1.09)  LDD1649  [26]
 LDCM0447  CL56 HEK-293T C170(0.93); C89(0.98); C136(0.95)  LDD1650  [26]
 LDCM0448  CL57 HEK-293T C170(0.88); C89(1.16)  LDD1651  [26]
 LDCM0449  CL58 HEK-293T C170(1.02); C89(0.81)  LDD1652  [26]
 LDCM0450  CL59 HEK-293T C170(0.95); C89(1.07)  LDD1653  [26]
 LDCM0451  CL6 HEK-293T C170(0.89); C89(1.12)  LDD1654  [26]
 LDCM0452  CL60 HEK-293T C170(1.21); C89(1.10)  LDD1655  [26]
 LDCM0453  CL61 HEK-293T C170(0.95); C89(1.03)  LDD1656  [26]
 LDCM0454  CL62 HEK-293T C170(1.01); C89(0.91)  LDD1657  [26]
 LDCM0455  CL63 HEK-293T C170(0.93); C89(0.92)  LDD1658  [26]
 LDCM0456  CL64 HEK-293T C170(0.97); C89(1.20)  LDD1659  [26]
 LDCM0457  CL65 HEK-293T C170(0.86); C89(1.04)  LDD1660  [26]
 LDCM0458  CL66 HEK-293T C170(0.78); C89(1.09)  LDD1661  [26]
 LDCM0459  CL67 HEK-293T C170(0.98); C89(1.04)  LDD1662  [26]
 LDCM0460  CL68 HEK-293T C170(0.94); C89(1.04); C136(0.95)  LDD1663  [26]
 LDCM0461  CL69 HEK-293T C170(0.98); C89(1.07)  LDD1664  [26]
 LDCM0462  CL7 HEK-293T C170(0.88); C89(0.94)  LDD1665  [26]
 LDCM0463  CL70 HEK-293T C170(0.94); C89(0.88)  LDD1666  [26]
 LDCM0464  CL71 HEK-293T C170(1.01); C89(1.01)  LDD1667  [26]
 LDCM0465  CL72 HEK-293T C170(1.00); C89(0.98)  LDD1668  [26]
 LDCM0466  CL73 HEK-293T C170(0.96); C89(1.08)  LDD1669  [26]
 LDCM0467  CL74 HEK-293T C170(0.94); C89(0.88)  LDD1670  [26]
 LDCM0469  CL76 HEK-293T C170(0.99); C89(1.00)  LDD1672  [26]
 LDCM0470  CL77 HEK-293T C170(0.89); C89(1.03)  LDD1673  [26]
 LDCM0471  CL78 HEK-293T C170(1.02); C89(1.15)  LDD1674  [26]
 LDCM0472  CL79 HEK-293T C170(0.87); C89(0.93)  LDD1675  [26]
 LDCM0473  CL8 HEK-293T C170(0.68); C89(1.34); C136(0.57)  LDD1676  [26]
 LDCM0474  CL80 HEK-293T C170(0.99); C89(1.06); C136(1.44)  LDD1677  [26]
 LDCM0475  CL81 HEK-293T C170(1.01); C89(1.19)  LDD1678  [26]
 LDCM0476  CL82 HEK-293T C170(1.10); C89(0.89)  LDD1679  [26]
 LDCM0477  CL83 HEK-293T C170(0.94); C89(1.11)  LDD1680  [26]
 LDCM0478  CL84 HEK-293T C170(1.07); C89(1.00)  LDD1681  [26]
 LDCM0479  CL85 HEK-293T C170(0.95); C89(1.13)  LDD1682  [26]
 LDCM0480  CL86 HEK-293T C170(0.87); C89(0.93)  LDD1683  [26]
 LDCM0481  CL87 HEK-293T C170(0.90); C89(0.92)  LDD1684  [26]
 LDCM0482  CL88 HEK-293T C170(0.88); C89(1.10)  LDD1685  [26]
 LDCM0483  CL89 HEK-293T C170(0.94); C89(1.16)  LDD1686  [26]
 LDCM0484  CL9 HEK-293T C170(0.97); C89(1.22)  LDD1687  [26]
 LDCM0485  CL90 HEK-293T C170(0.83); C89(1.21)  LDD1688  [26]
 LDCM0486  CL91 HEK-293T C170(0.89); C89(1.08)  LDD1689  [26]
 LDCM0487  CL92 HEK-293T C170(0.92); C89(1.10); C136(0.78)  LDD1690  [26]
 LDCM0488  CL93 HEK-293T C170(0.90); C89(1.11)  LDD1691  [26]
 LDCM0489  CL94 HEK-293T C170(1.04); C89(0.90)  LDD1692  [26]
 LDCM0490  CL95 HEK-293T C170(0.94); C89(1.26)  LDD1693  [26]
 LDCM0491  CL96 HEK-293T C170(0.97); C89(1.01)  LDD1694  [26]
 LDCM0492  CL97 HEK-293T C170(0.89); C89(1.05)  LDD1695  [26]
 LDCM0493  CL98 HEK-293T C170(0.93); C89(0.97)  LDD1696  [26]
 LDCM0494  CL99 HEK-293T C170(0.93); C89(0.87)  LDD1697  [26]
 LDCM0495  E2913 HEK-293T C170(0.96); C89(0.91)  LDD1698  [26]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C170(1.83)  LDD1702  [7]
 LDCM0625  F8 Ramos C170(1.00)  LDD2187  [27]
 LDCM0572  Fragment10 Ramos C170(0.67)  LDD2189  [27]
 LDCM0573  Fragment11 Ramos C170(0.09)  LDD2190  [27]
 LDCM0574  Fragment12 Ramos C170(0.92)  LDD2191  [27]
 LDCM0575  Fragment13 Ramos C170(1.09)  LDD2192  [27]
 LDCM0576  Fragment14 Ramos C170(0.72)  LDD2193  [27]
 LDCM0579  Fragment20 Ramos C170(0.66)  LDD2194  [27]
 LDCM0580  Fragment21 Ramos C170(1.11)  LDD2195  [27]
 LDCM0582  Fragment23 Ramos C170(0.40)  LDD2196  [27]
 LDCM0578  Fragment27 Ramos C170(1.22)  LDD2197  [27]
 LDCM0586  Fragment28 Ramos C170(0.99)  LDD2198  [27]
 LDCM0588  Fragment30 Ramos C170(0.99)  LDD2199  [27]
 LDCM0589  Fragment31 Ramos C170(1.13)  LDD2200  [27]
 LDCM0590  Fragment32 Ramos C170(0.62)  LDD2201  [27]
 LDCM0468  Fragment33 HEK-293T C170(0.95); C89(1.09)  LDD1671  [26]
 LDCM0596  Fragment38 Ramos C170(1.23)  LDD2203  [27]
 LDCM0566  Fragment4 Ramos C170(0.78)  LDD2184  [27]
 LDCM0427  Fragment51 HEK-293T C170(0.90); C89(0.88)  LDD1631  [26]
 LDCM0610  Fragment52 Ramos C170(1.15)  LDD2204  [27]
 LDCM0614  Fragment56 Ramos C170(1.08)  LDD2205  [27]
 LDCM0569  Fragment7 Ramos C170(0.84)  LDD2186  [27]
 LDCM0571  Fragment9 Ramos C170(0.62)  LDD2188  [27]
 LDCM0116  HHS-0101 DM93 Y34(1.01)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y34(0.73)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y34(1.10)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y34(0.71)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y34(1.04)  LDD0268  [8]
 LDCM0107  IAA HeLa N.A.  LDD0221  [22]
 LDCM0022  KB02 HEK-293T C170(0.98); C89(1.03)  LDD1492  [26]
 LDCM0023  KB03 HEK-293T C170(1.00); C89(1.13)  LDD1497  [26]
 LDCM0024  KB05 COLO792 C201(1.55)  LDD3310  [6]
 LDCM0109  NEM HeLa H200(0.00); H178(0.00)  LDD0223  [22]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C170(1.08)  LDD2125  [7]
 LDCM0131  RA190 MM1.R C170(1.47)  LDD0304  [28]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) PPP phosphatase family P67775
Zinc finger protein RFP (TRIM27) TRIM/RBCC family P14373
Tryptophan 2,3-dioxygenase (TDO2) Tryptophan 2,3-dioxygenase family P48775
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Eukaryotic translation initiation factor 4E transporter (EIF4ENIF1) 4E-T/EIF4E-T family Q9NRA8
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein EMX2 (EMX2) EMX homeobox family Q04743
Other
Click To Hide/Show 11 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1) EIF4E-binding protein family Q13541
Eukaryotic translation initiation factor 4E-binding protein 2 (EIF4EBP2) EIF4E-binding protein family Q13542
Eukaryotic translation initiation factor 4E-binding protein 3 (EIF4EBP3) EIF4E-binding protein family O60516
Eukaryotic translation initiation factor 4 gamma 1 (EIF4G1) Eukaryotic initiation factor 4G family Q04637
Eukaryotic translation initiation factor 4 gamma 3 (EIF4G3) Eukaryotic initiation factor 4G family O43432
Polyadenylate-binding protein 1 (PABPC1) Polyadenylate-binding protein type-1 family P11940
Small ubiquitin-related modifier 1 (SUMO1) Ubiquitin family P63165
Gem-associated protein 5 (GEMIN5) WD repeat gemin-5 family Q8TEQ6
KN motif and ankyrin repeat domain-containing protein 2 (KANK2) . Q63ZY3
Leucine-rich PPR motif-containing protein, mitochondrial (LRPPRC) . P42704
UBX domain-containing protein 11 (UBXN11) . Q5T124

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
7-methyl-gpppa Small molecular drug DB01649
7-methyl-guanosine-5'-triphosphate Small molecular drug DB02716
7-methyl-78-dihydroguanosine-5'-diphosphate . DB01960
Ly2275796 . DB05165
S-[(1-hydroxy-2255-tetramethyl-25-dihydro-1h-pyrrol-3-yl)Methyl] Methanesulfonothioate . DB08217

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 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.
3 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
4 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
5 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.
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
7 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
8 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.
9 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.
10 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
11 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.
12 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
13 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
14 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
15 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
16 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
17 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
18 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
19 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
20 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
21 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.
22 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.
23 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
24 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
25 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.
26 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
27 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
28 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.