Details of the Target

General Information of Target

Target ID LDTP08908
Target Name Ephexin-1 (NGEF)
Gene Name NGEF
Gene ID 25791
Synonyms
Ephexin-1; Eph-interacting exchange protein; Neuronal guanine nucleotide exchange factor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
METRESEDLEKTRRKSASDQWNTDNEPAKVKPELLPEKEETSQADQDIQDKEPHCHIPIK
RNSIFNRSIRRKSKAKARDNPERNASCLADSQDNGKSVNEPLTLNIPWSRMPPCRTAMQT
DPGAQEMSESSSTPGNGATPEEWPALADSPTTLTEALRMIHPIPADSWRNLIEQIGLLYQ
EYRDKSTLQEIETRRQQDAEIEDNTNGSPASEDTPEEEEEEEEEEEPASPPERKTLPQIC
LLSNPHSRFNLWQDLPEIRSSGVLEILQPEEIKLQEAMFELVTSEASYYKSLNLLVSHFM
ENERIRKILHPSEAHILFSNVLDVLAVSERFLLELEHRMEENIVISDVCDIVYRYAADHF
SVYITYVSNQTYQERTYKQLLQEKAAFRELIAQLELDPKCRGLPFSSFLILPFQRITRLK
LLVQNILKRVEERSERECTALDAHKELEMVVKACNEGVRKMSRTEQMISIQKKMEFKIKS
VPIISHSRWLLKQGELQQMSGPKTSRTLRTKKLFHEIYLFLFNDLLVICRQIPGDKYQVF
DSAPRGLLRVEELEDQGQTLANVFILRLLENADDREATYMLKASSQSEMKRWMTSLAPNR
RTKFVSFTSRLLDCPQVQCVHPYVAQQPDELTLELADILNILDKTDDGWIFGERLHDQER
GWFPSSMTEEILNPKIRSQNLKECFRVHKMDDPQRSQNKDRRKLGSRNRQ
Target Bioclass
Other
Subcellular location
Cytoplasm
Function
Acts as a guanine nucleotide exchange factor (GEF) which differentially activates the GTPases RHOA, RAC1 and CDC42. Plays a role in axon guidance regulating ephrin-induced growth cone collapse and dendritic spine morphogenesis. Upon activation by ephrin through EPHA4, the GEF activity switches toward RHOA resulting in its activation. Activated RHOA promotes cone retraction at the expense of RAC1- and CDC42-stimulated growth cone extension.
Uniprot ID
Q8N5V2
Ensemble ID
ENST00000264051.8
HGNC ID
HGNC:7807

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.E271K .
COLO678 SNV: p.E340G .
FTC133 SNV: p.E52K .
HCT15 SNV: p.P122T DBIA    Probe Info 
HT SNV: p.V367D .
KPNYN SNV: p.P144R .
MCC13 SNV: p.E37K .
MFE296 SNV: p.T235I .

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  		C454(3.34)  LDD3322  [1]
NAIA_4
 Probe Info  		N.A.  LDD2226  [2]
IPM
 Probe Info  		N.A.  LDD0005  [3]
AOyne
 Probe Info  		14.40  LDD0443  [4]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C106
 Probe Info  		19.70  LDD1793  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C240(1.09)  LDD1507  [6]
 LDCM0226  AC11 HEK-293T C454(1.14)  LDD1509  [6]
 LDCM0237  AC12 HEK-293T C454(1.16)  LDD1510  [6]
 LDCM0276  AC17 HEK-293T C240(1.01)  LDD1515  [6]
 LDCM0278  AC19 HEK-293T C454(1.18)  LDD1517  [6]
 LDCM0280  AC20 HEK-293T C454(1.09)  LDD1519  [6]
 LDCM0281  AC21 HEK-293T C454(1.02)  LDD1520  [6]
 LDCM0284  AC24 HEK-293T C454(1.02); C438(0.94)  LDD1523  [6]
 LDCM0285  AC25 HEK-293T C240(1.07)  LDD1524  [6]
 LDCM0287  AC27 HEK-293T C454(1.05)  LDD1526  [6]
 LDCM0288  AC28 HEK-293T C454(1.13)  LDD1527  [6]
 LDCM0289  AC29 HEK-293T C454(1.01)  LDD1528  [6]
 LDCM0290  AC3 HEK-293T C454(1.11)  LDD1529  [6]
 LDCM0293  AC32 HEK-293T C454(1.00); C438(0.95)  LDD1532  [6]
 LDCM0294  AC33 HEK-293T C240(0.91)  LDD1533  [6]
 LDCM0296  AC35 HEK-293T C454(1.10)  LDD1535  [6]
 LDCM0297  AC36 HEK-293T C454(1.17)  LDD1536  [6]
 LDCM0298  AC37 HEK-293T C454(1.04)  LDD1537  [6]
 LDCM0301  AC4 HEK-293T C454(1.17)  LDD1540  [6]
 LDCM0302  AC40 HEK-293T C454(0.88); C438(0.94)  LDD1541  [6]
 LDCM0303  AC41 HEK-293T C240(1.16)  LDD1542  [6]
 LDCM0305  AC43 HEK-293T C454(1.19)  LDD1544  [6]
 LDCM0306  AC44 HEK-293T C454(1.14)  LDD1545  [6]
 LDCM0307  AC45 HEK-293T C454(1.08)  LDD1546  [6]
 LDCM0310  AC48 HEK-293T C454(1.09); C438(0.95)  LDD1549  [6]
 LDCM0311  AC49 HEK-293T C240(0.91)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C454(1.03)  LDD1551  [6]
 LDCM0314  AC51 HEK-293T C454(1.02)  LDD1553  [6]
 LDCM0315  AC52 HEK-293T C454(1.15)  LDD1554  [6]
 LDCM0316  AC53 HEK-293T C454(1.11)  LDD1555  [6]
 LDCM0319  AC56 HEK-293T C454(1.07); C438(0.97)  LDD1558  [6]
 LDCM0320  AC57 HEK-293T C240(1.09)  LDD1559  [6]
 LDCM0322  AC59 HEK-293T C454(1.15)  LDD1561  [6]
 LDCM0324  AC60 HEK-293T C454(1.11)  LDD1563  [6]
 LDCM0325  AC61 HEK-293T C454(1.07)  LDD1564  [6]
 LDCM0328  AC64 HEK-293T C454(1.06); C438(0.93)  LDD1567  [6]
 LDCM0345  AC8 HEK-293T C454(0.86); C438(1.07)  LDD1569  [6]
 LDCM0248  AKOS034007472 HEK-293T C454(0.96)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C240(0.94)  LDD1570  [6]
 LDCM0275  AKOS034007705 HEK-293T C454(0.95); C438(0.99)  LDD1514  [6]
 LDCM0390  CL12 HEK-293T C454(1.10); C438(1.11)  LDD1594  [6]
 LDCM0404  CL17 HEK-293T C240(1.17)  LDD1608  [6]
 LDCM0406  CL19 HEK-293T C454(1.12)  LDD1610  [6]
 LDCM0408  CL20 HEK-293T C454(1.19)  LDD1612  [6]
 LDCM0409  CL21 HEK-293T C454(1.02)  LDD1613  [6]
 LDCM0412  CL24 HEK-293T C454(1.04); C438(1.14)  LDD1616  [6]
 LDCM0417  CL29 HEK-293T C240(0.98)  LDD1621  [6]
 LDCM0420  CL31 HEK-293T C454(1.24)  LDD1624  [6]
 LDCM0421  CL32 HEK-293T C454(1.27)  LDD1625  [6]
 LDCM0422  CL33 HEK-293T C454(1.11)  LDD1626  [6]
 LDCM0425  CL36 HEK-293T C454(1.01); C438(1.08)  LDD1629  [6]
 LDCM0431  CL41 HEK-293T C240(1.14)  LDD1635  [6]
 LDCM0433  CL43 HEK-293T C454(1.08)  LDD1637  [6]
 LDCM0434  CL44 HEK-293T C454(1.09)  LDD1638  [6]
 LDCM0435  CL45 HEK-293T C454(1.22)  LDD1639  [6]
 LDCM0438  CL48 HEK-293T C454(1.29); C438(1.00)  LDD1642  [6]
 LDCM0440  CL5 HEK-293T C240(1.22)  LDD1644  [6]
 LDCM0444  CL53 HEK-293T C240(1.12)  LDD1647  [6]
 LDCM0446  CL55 HEK-293T C454(1.10)  LDD1649  [6]
 LDCM0447  CL56 HEK-293T C454(1.31)  LDD1650  [6]
 LDCM0448  CL57 HEK-293T C454(1.22)  LDD1651  [6]
 LDCM0452  CL60 HEK-293T C454(1.01); C438(0.95)  LDD1655  [6]
 LDCM0457  CL65 HEK-293T C240(1.12)  LDD1660  [6]
 LDCM0459  CL67 HEK-293T C454(1.18)  LDD1662  [6]
 LDCM0460  CL68 HEK-293T C454(1.20)  LDD1663  [6]
 LDCM0461  CL69 HEK-293T C454(1.08)  LDD1664  [6]
 LDCM0462  CL7 HEK-293T C454(1.17)  LDD1665  [6]
 LDCM0465  CL72 HEK-293T C454(1.20); C438(1.12)  LDD1668  [6]
 LDCM0470  CL77 HEK-293T C240(1.16)  LDD1673  [6]
 LDCM0472  CL79 HEK-293T C454(1.13)  LDD1675  [6]
 LDCM0473  CL8 HEK-293T C454(1.10)  LDD1676  [6]
 LDCM0474  CL80 HEK-293T C454(1.20)  LDD1677  [6]
 LDCM0475  CL81 HEK-293T C454(1.13)  LDD1678  [6]
 LDCM0478  CL84 HEK-293T C454(0.99); C438(1.07)  LDD1681  [6]
 LDCM0483  CL89 HEK-293T C240(1.12)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C454(1.10)  LDD1687  [6]
 LDCM0486  CL91 HEK-293T C454(1.11)  LDD1689  [6]
 LDCM0487  CL92 HEK-293T C454(1.22)  LDD1690  [6]
 LDCM0488  CL93 HEK-293T C454(1.07)  LDD1691  [6]
 LDCM0491  CL96 HEK-293T C454(1.19); C438(0.91)  LDD1694  [6]
 LDCM0022  KB02 42-MG-BA C438(1.03)  LDD2244  [1]
 LDCM0023  KB03 42-MG-BA C438(1.24)  LDD2661  [1]
 LDCM0024  KB05 SKMEL2 C454(3.34)  LDD3322  [1]

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
Fibroblast growth factor receptor 3 (FGFR3) Tyr protein kinase family P22607
GTPase HRas (HRAS) Ras family P01112
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Wolframin (WFS1) . O76024
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Progranulin (GRN) Granulin family P28799
Heat shock protein beta-1 (HSPB1) Small heat shock protein (HSP20) family P04792
Gelsolin (GSN) Villin/gelsolin family P06396
RING finger protein 11 (RNF11) . Q9Y3C5

References

1 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
2 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
3 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
4 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.
5 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
6 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