Details of the Target

General Information of Target

Target ID LDTP06564
Target Name Mitogen-activated protein kinase kinase kinase 11 (MAP3K11)
Gene Name MAP3K11
Gene ID 4296
Synonyms
MLK3; PTK1; SPRK; Mitogen-activated protein kinase kinase kinase 11; EC 2.7.11.25; Mixed lineage kinase 3; Src-homology 3 domain-containing proline-rich kinase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEPLKSLFLKSPLGSWNGSGSGGGGGGGGGRPEGSPKAAGYANPVWTALFDYEPSGQDEL
ALRKGDRVEVLSRDAAISGDEGWWAGQVGGQVGIFPSNYVSRGGGPPPCEVASFQELRLE
EVIGIGGFGKVYRGSWRGELVAVKAARQDPDEDISVTAESVRQEARLFAMLAHPNIIALK
AVCLEEPNLCLVMEYAAGGPLSRALAGRRVPPHVLVNWAVQIARGMHYLHCEALVPVIHR
DLKSNNILLLQPIESDDMEHKTLKITDFGLAREWHKTTQMSAAGTYAWMAPEVIKASTFS
KGSDVWSFGVLLWELLTGEVPYRGIDCLAVAYGVAVNKLTLPIPSTCPEPFAQLMADCWA
QDPHRRPDFASILQQLEALEAQVLREMPRDSFHSMQEGWKREIQGLFDELRAKEKELLSR
EEELTRAAREQRSQAEQLRRREHLLAQWELEVFERELTLLLQQVDRERPHVRRRRGTFKR
SKLRARDGGERISMPLDFKHRITVQASPGLDRRRNVFEVGPGDSPTFPRFRAIQLEPAEP
GQAWGRQSPRRLEDSSNGERRACWAWGPSSPKPGEAQNGRRRSRMDEATWYLDSDDSSPL
GSPSTPPALNGNPPRPSLEPEEPKRPVPAERGSSSGTPKLIQRALLRGTALLASLGLGRD
LQPPGGPGRERGESPTTPPTPTPAPCPTEPPPSPLICFSLKTPDSPPTPAPLLLDLGIPV
GQRSAKSPRREEEPRGGTVSPPPGTSRSAPGTPGTPRSPPLGLISRPRPSPLRSRIDPWS
FVSAGPRPSPLPSPQPAPRRAPWTLFPDSDPFWDSPPANPFQGGPQDCRAQTKDMGAQAP
WVPEAGP
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase kinase subfamily
Subcellular location
Cytoplasm, cytoskeleton, microtubule organizing center, centrosome
Function
Activates the JUN N-terminal pathway. Required for serum-stimulated cell proliferation and for mitogen and cytokine activation of MAPK14 (p38), MAPK3 (ERK) and MAPK8 (JNK1) through phosphorylation and activation of MAP2K4/MKK4 and MAP2K7/MKK7. Plays a role in mitogen-stimulated phosphorylation and activation of BRAF, but does not phosphorylate BRAF directly. Influences microtubule organization during the cell cycle.
TTD ID
T12126
Uniprot ID
Q16584
DrugMap ID
TTETX6Q
Ensemble ID
ENST00000309100.8
HGNC ID
HGNC:6850
ChEMBL ID
CHEMBL2708

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.R385W .
HEC1B SNV: p.R385W; p.R723W .
HT SNV: p.G648A .
Ishikawa (Heraklio) 02 ER SNV: p.Q437P .
JURKAT SNV: p.R432W .
MDST8 SNV: p.S569T .
MELHO SNV: p.P771S .
MOLT4 Deletion: p.G824AfsTer123
SNV: p.S524L;p.A818P		 .
NCIH358 SNV: p.I177T .
REH SNV: p.S524L .
SKMEL2 SNV: p.E121D .
SKMEL24 Substitution: p.P692S .
SNU245 SNV: p.S602C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C563(8.18)  LDD0315  [1]
DBIA
 Probe Info  		C327(0.97)  LDD1514  [2]
NAIA_5
 Probe Info  		N.A.  LDD2224  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0284  AC24 HEK-293T C327(1.09)  LDD1523  [2]
 LDCM0293  AC32 HEK-293T C327(0.97)  LDD1532  [2]
 LDCM0302  AC40 HEK-293T C327(1.14)  LDD1541  [2]
 LDCM0310  AC48 HEK-293T C327(0.96)  LDD1549  [2]
 LDCM0319  AC56 HEK-293T C327(0.92)  LDD1558  [2]
 LDCM0328  AC64 HEK-293T C327(1.23)  LDD1567  [2]
 LDCM0345  AC8 HEK-293T C327(1.03)  LDD1569  [2]
 LDCM0275  AKOS034007705 HEK-293T C327(0.97)  LDD1514  [2]
 LDCM0632  CL-Sc Hep-G2 C563(0.19)  LDD2227  [3]
 LDCM0369  CL100 HEK-293T C563(1.05)  LDD1573  [2]
 LDCM0371  CL102 HEK-293T C563(0.86)  LDD1575  [2]
 LDCM0372  CL103 HEK-293T C563(0.91)  LDD1576  [2]
 LDCM0373  CL104 HEK-293T C563(1.05)  LDD1577  [2]
 LDCM0375  CL106 HEK-293T C563(0.94)  LDD1579  [2]
 LDCM0376  CL107 HEK-293T C563(0.82)  LDD1580  [2]
 LDCM0377  CL108 HEK-293T C563(0.88)  LDD1581  [2]
 LDCM0380  CL110 HEK-293T C563(0.76)  LDD1584  [2]
 LDCM0381  CL111 HEK-293T C563(1.08)  LDD1585  [2]
 LDCM0382  CL112 HEK-293T C563(1.02)  LDD1586  [2]
 LDCM0384  CL114 HEK-293T C563(1.48)  LDD1588  [2]
 LDCM0385  CL115 HEK-293T C563(1.05)  LDD1589  [2]
 LDCM0386  CL116 HEK-293T C563(1.22)  LDD1590  [2]
 LDCM0388  CL118 HEK-293T C563(0.93)  LDD1592  [2]
 LDCM0389  CL119 HEK-293T C563(1.17)  LDD1593  [2]
 LDCM0390  CL12 HEK-293T C327(1.07)  LDD1594  [2]
 LDCM0391  CL120 HEK-293T C563(1.06)  LDD1595  [2]
 LDCM0393  CL122 HEK-293T C563(0.94)  LDD1597  [2]
 LDCM0394  CL123 HEK-293T C563(0.86)  LDD1598  [2]
 LDCM0395  CL124 HEK-293T C563(1.11)  LDD1599  [2]
 LDCM0397  CL126 HEK-293T C563(0.79)  LDD1601  [2]
 LDCM0398  CL127 HEK-293T C563(0.87)  LDD1602  [2]
 LDCM0399  CL128 HEK-293T C563(0.90)  LDD1603  [2]
 LDCM0401  CL14 HEK-293T C563(1.17)  LDD1605  [2]
 LDCM0402  CL15 HEK-293T C563(1.07)  LDD1606  [2]
 LDCM0403  CL16 HEK-293T C563(1.06)  LDD1607  [2]
 LDCM0407  CL2 HEK-293T C563(1.09)  LDD1611  [2]
 LDCM0412  CL24 HEK-293T C327(1.03)  LDD1616  [2]
 LDCM0414  CL26 HEK-293T C563(1.15)  LDD1618  [2]
 LDCM0415  CL27 HEK-293T C563(1.01)  LDD1619  [2]
 LDCM0416  CL28 HEK-293T C563(0.94)  LDD1620  [2]
 LDCM0418  CL3 HEK-293T C563(0.54)  LDD1622  [2]
 LDCM0425  CL36 HEK-293T C327(0.91)  LDD1629  [2]
 LDCM0428  CL39 HEK-293T C563(1.13)  LDD1632  [2]
 LDCM0429  CL4 HEK-293T C563(0.93)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C563(0.98)  LDD1634  [2]
 LDCM0438  CL48 HEK-293T C327(0.94)  LDD1642  [2]
 LDCM0441  CL50 HEK-293T C563(0.94)  LDD1645  [2]
 LDCM0443  CL52 HEK-293T C563(0.94)  LDD1646  [2]
 LDCM0452  CL60 HEK-293T C327(1.10)  LDD1655  [2]
 LDCM0454  CL62 HEK-293T C563(1.20)  LDD1657  [2]
 LDCM0455  CL63 HEK-293T C563(1.07)  LDD1658  [2]
 LDCM0456  CL64 HEK-293T C563(0.80)  LDD1659  [2]
 LDCM0465  CL72 HEK-293T C327(0.91)  LDD1668  [2]
 LDCM0467  CL74 HEK-293T C563(0.91)  LDD1670  [2]
 LDCM0469  CL76 HEK-293T C563(1.06)  LDD1672  [2]
 LDCM0478  CL84 HEK-293T C327(1.09)  LDD1681  [2]
 LDCM0480  CL86 HEK-293T C563(1.04)  LDD1683  [2]
 LDCM0481  CL87 HEK-293T C563(0.95)  LDD1684  [2]
 LDCM0482  CL88 HEK-293T C563(0.92)  LDD1685  [2]
 LDCM0491  CL96 HEK-293T C327(1.12)  LDD1694  [2]
 LDCM0493  CL98 HEK-293T C563(1.08)  LDD1696  [2]
 LDCM0494  CL99 HEK-293T C563(0.99)  LDD1697  [2]
 LDCM0495  E2913 HEK-293T C563(0.92)  LDD1698  [2]
 LDCM0468  Fragment33 HEK-293T C563(0.91)  LDD1671  [2]
 LDCM0427  Fragment51 HEK-293T C563(0.92)  LDD1631  [2]
 LDCM0023  KB03 Jurkat C563(8.18)  LDD0315  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cell division control protein 42 homolog (CDC42) Rho family P60953
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Merlin (NF2) . P35240

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cep-5104 Small molecular drug D09QBA
Cep-6331 Small molecular drug D07IHM
Pmid24044867c8 Small molecular drug D0YQ8V
Urmc-099 Small molecular drug D07ADX
Cep1349 . D0O7HD

References

1 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
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
3 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