General Information of Target

Target ID LDTP05157
Target Name Mitogen-activated protein kinase kinase kinase 9 (MAP3K9)
Gene Name MAP3K9
Gene ID 4293
Synonyms
MLK1; PRKE1; Mitogen-activated protein kinase kinase kinase 9; EC 2.7.11.25; Mixed lineage kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEPSRALLGCLASAAAAAPPGEDGAGAGAEEEEEEEEEAAAAVGPGELGCDAPLPYWTAV
FEYEAAGEDELTLRLGDVVEVLSKDSQVSGDEGWWTGQLNQRVGIFPSNYVTPRSAFSSR
CQPGGEDPSCYPPIQLLEIDFAELTLEEIIGIGGFGKVYRAFWIGDEVAVKAARHDPDED
ISQTIENVRQEAKLFAMLKHPNIIALRGVCLKEPNLCLVMEFARGGPLNRVLSGKRIPPD
ILVNWAVQIARGMNYLHDEAIVPIIHRDLKSSNILILQKVENGDLSNKILKITDFGLARE
WHRTTKMSAAGTYAWMAPEVIRASMFSKGSDVWSYGVLLWELLTGEVPFRGIDGLAVAYG
VAMNKLALPIPSTCPEPFAKLMEDCWNPDPHSRPSFTNILDQLTTIEESGFFEMPKDSFH
CLQDNWKHEIQEMFDQLRAKEKELRTWEEELTRAALQQKNQEELLRRREQELAEREIDIL
ERELNIIIHQLCQEKPRVKKRKGKFRKSRLKLKDGNRISLPSDFQHKFTVQASPTMDKRK
SLINSRSSPPASPTIIPRLRAIQLTPGESSKTWGRSSVVPKEEGEEEEKRAPKKKGRTWG
PGTLGQKELASGDEGSPQRREKANGLSTPSESPHFHLGLKSLVDGYKQWSSSAPNLVKGP
RSSPALPGFTSLMEMEDEDSEGPGSGESRLQHSPSQSYLCIPFPRGEDGDGPSSDGIHEE
PTPVNSATSTPQLTPTNSLKRGGAHHRRCEVALLGCGAVLAATGLGFDLLEAGKCQLLPL
EEPEPPAREEKKRREGLFQRSSRPRRSTSPPSRKLFKKEEPMLLLGDPSASLTLLSLSSI
SECNSTRSLLRSDSDEIVVYEMPVSPVEAPPLSPCTHNPLVNVRVERFKRDPNQSLTPTH
VTLTTPSQPSSHRRTPSDGALKPETLLASRSPSSNGLSPSPGAGMLKTPSPSRDPGEFPR
LPDPNVVFPPTPRRWNTQQDSTLERPKTLEFLPRPRPSANRQRLDPWWFVSPSHARSTSP
ANSSSTETPSNLDSCFASSSSTVEERPGLPALLPFQAGPLPPTERTLLDLDAEGQSQDST
VPLCRAELNTHRPAPYEIQQEFWS
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase kinase subfamily
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. Plays an important role in the cascades of cellular responses evoked by changes in the environment. Once activated, acts as an upstream activator of the MKK/JNK signal transduction cascade through the phosphorylation of MAP2K4/MKK4 and MAP2K7/MKK7 which in turn activate the JNKs. The MKK/JNK signaling pathway regulates stress response via activator protein-1 (JUN) and GATA4 transcription factors. Also plays a role in mitochondrial death signaling pathway, including the release cytochrome c, leading to apoptosis.
TTD ID
T19760
Uniprot ID
P80192
DrugMap ID
TTUNSIX
Ensemble ID
ENST00000554752.7
HGNC ID
HGNC:6861
ChEMBL ID
CHEMBL2872

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 SNV: p.P810S .
COLO792 SNV: p.M414L .
COLO800 SNV: p.A761P .
DU145 SNV: p.A16T .
ETK1 SNV: p.V79G .
FADU Deletion: p.I479MfsTer17 .
FTC133 SNV: p.T312M .
HCT15 SNV: p.Q423Ter .
HGC27 SNV: p.E924G .
HT115 SNV: p.D353G .
IGROV1 SNV: p.V320F .
JURKAT SNV: p.T1026I .
KARPAS422 Insertion: p.S950QfsTer8 .
L428 SNV: p.N844Y .
LN229 SNV: p.L194R .
LS123 SNV: p.H745P .
MDAMB231 SNV: p.S1079N .
MEWO SNV: p.E376G; p.P388S; p.R560Ter .
MFE296 SNV: p.A310T .
NALM6 SNV: p.R509L .
OVCAR5 SNV: p.S118P .
OVK18 SNV: p.Q908Ter .
SKMEL2 SNV: p.L815F .
SKMEL24 SNV: p.P731S .
TOV21G SNV: p.E449Ter; p.G684W .

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
Acrolein
 Probe Info 
N.A.  LDD0222  [1]
W1
 Probe Info 
D435(0.00); E432(0.00); R438(0.00)  LDD0236  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [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
Histone acetyltransferase KAT5 (KAT5) MYST (SAS/MOZ) family Q92993
Protein kinase C alpha type (PRKCA) AGC Ser/Thr protein kinase family P17252
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein gamma (YWHAG) 14-3-3 family P61981
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238

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
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cep1347 Small molecular drug D03QLG
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cep-5104 Small molecular drug D09QBA
Cep-6331 Small molecular drug D07IHM
Urmc-099 Small molecular drug D07ADX
12-(2-hydroxyethyl)-2-(1-methylethoxy)-1314-dihydronaphtho[21-a]Pyrrolo[34-c]Carbazol-5(12h)-one . DB08703

References

1 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.
2 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.