General Information of Target

Target ID LDTP13493
Target Name Guanine nucleotide exchange factor VAV3 (VAV3)
Gene Name VAV3
Gene ID 10451
Synonyms
Guanine nucleotide exchange factor VAV3; VAV-3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MYSGAGPALAPPAPPPPIQGYAFKPPPRPDFGTSGRTIKLQANFFEMDIPKIDIYHYELD
IKPEKCPRRVNREIVEHMVQHFKTQIFGDRKPVFDGRKNLYTAMPLPIGRDKVELEVTLP
GEGKDRIFKVSIKWVSCVSLQALHDALSGRLPSVPFETIQALDVVMRHLPSMRYTPVGRS
FFTASEGCSNPLGGGREVWFGFHQSVRPSLWKMMLNIDVSATAFYKAQPVIEFVCEVLDF
KSIEEQQKPLTDSQRVKFTKEIKGLKVEITHCGQMKRKYRVCNVTRRPASHQTFPLQQES
GQTVECTVAQYFKDRHKLVLRYPHLPCLQVGQEQKHTYLPLEVCNIVAGQRCIKKLTDNQ
TSTMIRATARSAPDRQEEISKLMRSASFNTDPYVREFGIMVKDEMTDVTGRVLQPPSILY
GGRNKAIATPVQGVWDMRNKQFHTGIEIKVWAIACFAPQRQCTEVHLKSFTEQLRKISRD
AGMPIQGQPCFCKYAQGADSVEPMFRHLKNTYAGLQLVVVILPGKTPVYAEVKRVGDTVL
GMATQCVQMKNVQRTTPQTLSNLCLKINVKLGGVNNILLPQGRPPVFQQPVIFLGADVTH
PPAGDGKKPSIAAVVGSMDAHPNRYCATVRVQQHRQEIIQDLAAMVRELLIQFYKSTRFK
PTRIIFYRDGVSEGQFQQVLHHELLAIREACIKLEKDYQPGITFIVVQKRHHTRLFCTDK
NERVGKSGNIPAGTTVDTKITHPTEFDFYLCSHAGIQGTSRPSHYHVLWDDNRFSSDELQ
ILTYQLCHTYVRCTRSVSIPAPAYYAHLVAFRARYHLVDKEHDSAEGSHTSGQSNGRDHQ
ALAKAVQVHQDTLRTMYFA
Target Bioclass
Other
Function
Exchange factor for GTP-binding proteins RhoA, RhoG and, to a lesser extent, Rac1. Binds physically to the nucleotide-free states of those GTPases. Plays an important role in angiogenesis. Its recruitment by phosphorylated EPHA2 is critical for EFNA1-induced RAC1 GTPase activation and vascular endothelial cell migration and assembly. May be important for integrin-mediated signaling, at least in some cell types. In osteoclasts, along with SYK tyrosine kinase, required for signaling through integrin alpha-v/beta-1 (ITAGV-ITGB1), a crucial event for osteoclast proper cytoskeleton organization and function. This signaling pathway involves RAC1, but not RHO, activation. Necessary for proper wound healing. In the course of wound healing, required for the phagocytotic cup formation preceding macrophage phagocytosis of apoptotic neutrophils. Responsible for integrin beta-2 (ITGB2)-mediated macrophage adhesion and, to a lesser extent, contributes to beta-3 (ITGB3)-mediated adhesion. Does not affect integrin beta-1 (ITGB1)-mediated adhesion.
Uniprot ID
Q9UKW4
Ensemble ID
ENST00000370056.9
HGNC ID
HGNC:12659

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 SNV: p.V690I .
COLO792 SNV: p.M361I .
HCC1143 SNV: p.Q385Ter .
HCT116 SNV: p.W837Ter .
HCT15 SNV: p.T346I; p.A773T .
LS180 SNV: p.L57P .
MFE319 SNV: p.T416A .
NCIH1666 SNV: p.A551E .
NCIH2291 SNV: p.L47I .
NCIH358 SNV: p.A621D .
ONS76 SNV: p.R640I DBIA    Probe Info 
RKO SNV: p.D254G .
TYKNU SNV: p.G648Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C83(5.11)  LDD0209  [1]
4-Iodoacetamidophenylacetylene
 Probe Info 
C187(0.00); C44(0.00); C71(0.00); C544(0.00)  LDD0038  [2]
IA-alkyne
 Probe Info 
C187(0.00); C44(0.00); C71(0.00); C544(0.00)  LDD0036  [2]
Lodoacetamide azide
 Probe Info 
C187(0.00); C44(0.00); C71(0.00); C309(0.00)  LDD0037  [2]
IPM
 Probe Info 
N.A.  LDD0147  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 697 C828(1.52); C530(1.00)  LDD2245  [4]
 LDCM0023  KB03 Jurkat C83(5.11)  LDD0209  [1]
 LDCM0024  KB05 MOLM-16 C828(2.72)  LDD3334  [4]

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
Ubiquitin thioesterase ZRANB1 (ZRANB1) Peptidase C64 family Q9UGI0
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
E3 ubiquitin-protein ligase CBL-B (CBLB) . Q13191
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) PI3K p85 subunit family P27986
RAD50-interacting protein 1 (RINT1) RINT1 family Q6NUQ1

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 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 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