Details of the Target

General Information of Target

Target ID LDTP02789
Target Name Proto-oncogene vav (VAV1)
Gene Name VAV1
Gene ID 7409
Synonyms
VAV; Proto-oncogene vav
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELWRQCTHWLIQCRVLPPSHRVTWDGAQVCELAQALRDGVLLCQLLNNLLPHAINLREV
NLRPQMSQFLCLKNIRTFLSTCCEKFGLKRSELFEAFDLFDVQDFGKVIYTLSALSWTPI
AQNRGIMPFPTEEESVGDEDIYSGLSDQIDDTVEEDEDLYDCVENEEAEGDEIYEDLMRS
EPVSMPPKMTEYDKRCCCLREIQQTEEKYTDTLGSIQQHFLKPLQRFLKPQDIEIIFINI
EDLLRVHTHFLKEMKEALGTPGAANLYQVFIKYKERFLVYGRYCSQVESASKHLDRVAAA
REDVQMKLEECSQRANNGRFTLRDLLMVPMQRVLKYHLLLQELVKHTQEAMEKENLRLAL
DAMRDLAQCVNEVKRDNETLRQITNFQLSIENLDQSLAHYGRPKIDGELKITSVERRSKM
DRYAFLLDKALLICKRRGDSYDLKDFVNLHSFQVRDDSSGDRDNKKWSHMFLLIEDQGAQ
GYELFFKTRELKKKWMEQFEMAISNIYPENATANGHDFQMFSFEETTSCKACQMLLRGTF
YQGYRCHRCRASAHKECLGRVPPCGRHGQDFPGTMKKDKLHRRAQDKKRNELGLPKMEVF
QEYYGLPPPPGAIGPFLRLNPGDIVELTKAEAEQNWWEGRNTSTNEIGWFPCNRVKPYVH
GPPQDLSVHLWYAGPMERAGAESILANRSDGTFLVRQRVKDAAEFAISIKYNVEVKHIKI
MTAEGLYRITEKKAFRGLTELVEFYQQNSLKDCFKSLDTTLQFPFKEPEKRTISRPAVGS
TKYFGTAKARYDFCARDRSELSLKEGDIIKILNKKGQQGWWRGEIYGRVGWFPANYVEED
YSEYC
Target Bioclass
Other
Function Couples tyrosine kinase signals with the activation of the Rho/Rac GTPases, thus leading to cell differentiation and/or proliferation.
Uniprot ID
P15498
Ensemble ID
ENST00000596764.5
HGNC ID
HGNC:12657
ChEMBL ID
CHEMBL3259472

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CORL88 Deletion: p.M254IfsTer53 .
HCT15 SNV: p.L322M .
IGR1 SNV: p.M501I .
KELLY SNV: p.T152M .
KMRC3 SNV: p.R357L .
LNCaP clone FGC SNV: p.R402W .
MCC26 SNV: p.A34V .
NCIH2172 SNV: p.R790C .
REH SNV: p.E824K DBIA    Probe Info 
SHP77 SNV: p.R828L .
TE4 SNV: p.C794Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C71(31.85)  LDD0209  [1]
4-Iodoacetamidophenylacetylene
 Probe Info  		C532(0.00); C44(0.00); C369(0.00); C71(0.00)  LDD0038  [2]
IA-alkyne
 Probe Info  		C532(0.00); C794(0.00); C44(0.00); C71(0.00)  LDD0036  [2]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [3]
Lodoacetamide azide
 Probe Info  		C532(0.00); C794(0.00); C44(0.00); C369(0.00)  LDD0037  [2]
Compound 10
 Probe Info  		C652(0.00); C71(0.00)  LDD2216  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0625  F8 Ramos C311(1.14); C284(1.17); C794(1.40); C369(0.47)  LDD2187  [5]
 LDCM0572  Fragment10 Ramos C311(0.68); C284(0.56); C794(1.53); C652(0.59)  LDD2189  [5]
 LDCM0573  Fragment11 Ramos C311(20.00); C284(0.71); C794(9.72); C369(0.17)  LDD2190  [5]
 LDCM0574  Fragment12 Ramos C311(0.66); C284(1.07); C794(1.53); C652(0.52)  LDD2191  [5]
 LDCM0575  Fragment13 Ramos C311(0.99); C284(0.86); C794(0.80); C652(0.71)  LDD2192  [5]
 LDCM0576  Fragment14 Ramos C311(1.12); C284(0.64); C794(0.38); C369(0.56)  LDD2193  [5]
 LDCM0579  Fragment20 Ramos C311(0.65); C284(0.71); C794(0.88); C652(0.50)  LDD2194  [5]
 LDCM0580  Fragment21 Ramos C311(0.90); C284(0.85); C652(0.94); C71(0.93)  LDD2195  [5]
 LDCM0582  Fragment23 Ramos C311(0.46); C284(0.70); C652(2.18); C71(0.61)  LDD2196  [5]
 LDCM0578  Fragment27 Ramos C311(0.90); C284(0.90); C794(1.73); C652(0.89)  LDD2197  [5]
 LDCM0586  Fragment28 Ramos C311(0.51); C284(0.42); C794(0.50); C71(1.03)  LDD2198  [5]
 LDCM0588  Fragment30 Ramos C311(1.17); C284(1.17); C794(1.03); C652(1.04)  LDD2199  [5]
 LDCM0589  Fragment31 Ramos C311(1.19); C284(1.32); C794(1.18)  LDD2200  [5]
 LDCM0590  Fragment32 Ramos C311(0.72); C284(1.05); C794(1.75); C652(0.57)  LDD2201  [5]
 LDCM0468  Fragment33 Ramos C311(1.17); C284(1.17); C794(1.51); C652(0.84)  LDD2202  [5]
 LDCM0596  Fragment38 Ramos C311(1.09); C284(1.09); C794(1.31); C652(0.61)  LDD2203  [5]
 LDCM0566  Fragment4 Ramos C311(0.88); C284(0.87); C794(0.74); C369(0.49)  LDD2184  [5]
 LDCM0610  Fragment52 Ramos C311(1.36); C284(1.09); C794(1.30); C652(0.69)  LDD2204  [5]
 LDCM0614  Fragment56 Ramos C311(1.36); C284(2.42); C794(1.29); C652(0.90)  LDD2205  [5]
 LDCM0569  Fragment7 Ramos C311(0.87); C284(0.71); C794(0.77); C369(0.40)  LDD2186  [5]
 LDCM0571  Fragment9 Ramos C311(0.65); C284(0.58); C794(1.14); C652(0.57)  LDD2188  [5]
 LDCM0022  KB02 Ramos C311(1.05); C284(0.52); C794(1.18); C369(0.40)  LDD2182  [5]
 LDCM0023  KB03 Jurkat C71(31.85)  LDD0209  [1]
 LDCM0024  KB05 UACC257 C652(1.23)  LDD3325  [6]
 LDCM0131  RA190 MM1.R C652(1.36)  LDD0304  [7]

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
Tyrosine-protein kinase ABL1 (ABL1) Tyr protein kinase family P00519
Ras-related C3 botulinum toxin substrate 1 (RAC1) Rho family P63000
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 655 (ZNF655) Krueppel C2H2-type zinc-finger protein family Q8N720
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Abl interactor 1 (ABI1) ABI family Q8IZP0
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
KH domain-containing, RNA-binding, signal transduction-associated protein 1 (KHDRBS1) KHDRBS family Q07666
Lymphocyte cytosolic protein 2 (LCP2) . Q13094
SH3 domain-binding protein 2 (SH3BP2) . P78314

References

1 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
2 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
3 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
4 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
5 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
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 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.