Details of the Target

General Information of Target

Target ID LDTP02076
Target Name Integrin beta-3 (ITGB3)
Gene Name ITGB3
Gene ID 3690
Synonyms
GP3A; Integrin beta-3; Platelet membrane glycoprotein IIIa; GPIIIa; CD antigen CD61
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRARPRPRPLWATVLALGALAGVGVGGPNICTTRGVSSCQQCLAVSPMCAWCSDEALPLG
SPRCDLKENLLKDNCAPESIEFPVSEARVLEDRPLSDKGSGDSSQVTQVSPQRIALRLRP
DDSKNFSIQVRQVEDYPVDIYYLMDLSYSMKDDLWSIQNLGTKLATQMRKLTSNLRIGFG
AFVDKPVSPYMYISPPEALENPCYDMKTTCLPMFGYKHVLTLTDQVTRFNEEVKKQSVSR
NRDAPEGGFDAIMQATVCDEKIGWRNDASHLLVFTTDAKTHIALDGRLAGIVQPNDGQCH
VGSDNHYSASTTMDYPSLGLMTEKLSQKNINLIFAVTENVVNLYQNYSELIPGTTVGVLS
MDSSNVLQLIVDAYGKIRSKVELEVRDLPEELSLSFNATCLNNEVIPGLKSCMGLKIGDT
VSFSIEAKVRGCPQEKEKSFTIKPVGFKDSLIVQVTFDCDCACQAQAEPNSHRCNNGNGT
FECGVCRCGPGWLGSQCECSEEDYRPSQQDECSPREGQPVCSQRGECLCGQCVCHSSDFG
KITGKYCECDDFSCVRYKGEMCSGHGQCSCGDCLCDSDWTGYYCNCTTRTDTCMSSNGLL
CSGRGKCECGSCVCIQPGSYGDTCEKCPTCPDACTFKKECVECKKFDRGALHDENTCNRY
CRDEIESVKELKDTGKDAVNCTYKNEDDCVVRFQYYEDSSGKSILYVVEEPECPKGPDIL
VVLLSVMGAILLIGLAALLIWKLLITIHDRKEFAKFEEERARAKWDTANNPLYKEATSTF
TNITYRGT
Target Type
Literature-reported
Target Bioclass
Other
Family
Integrin beta chain family
Subcellular location
Cell membrane
Function
Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha-V/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha-IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets. ITGAV:ITGB3 binds to fractalkine (CX3CL1) and acts as its coreceptor in CX3CR1-dependent fractalkine signaling. ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling. ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling. ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling. ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling. ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling. ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling. ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1. ITGAV:ITGB3 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1. In brain, plays a role in synaptic transmission and plasticity. Involved in the regulation of the serotonin neurotransmission, is required to localize to specific compartments within the synapse the serotonin receptor SLC6A4 and for an appropriate reuptake of serotonin. Controls excitatory synaptic strength by regulating GRIA2-containing AMPAR endocytosis, which affects AMPAR abundance and composition. ITGAV:ITGB3 act as a receptor for CD40LG. ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP.; (Microbial infection) Integrin ITGAV:ITGB3 acts as a receptor for Herpes virus 8/HHV-8.; (Microbial infection) Integrin ITGAV:ITGB3 acts as a receptor for Coxsackievirus A9.; (Microbial infection) Acts as a receptor for Hantaan virus.; (Microbial infection) Integrin ITGAV:ITGB3 acts as a receptor for Cytomegalovirus/HHV-5.; (Microbial infection) Integrin ITGA5:ITGB3 acts as a receptor for Human metapneumovirus.; (Microbial infection) Integrin ITGAV:ITGB3 acts aP05556s a receptor for Human parechovirus 1.; (Microbial infection) Integrin ITGAV:ITGB3 acts as a receptor for West nile virus.; (Microbial infection) In case of HIV-1 infection, the interaction with extracellular viral Tat protein seems to enhance angiogenesis in Kaposi's sarcoma lesions.
TTD ID
T26457
Uniprot ID
P05106
DrugMap ID
TT8NBXR
Ensemble ID
ENST00000559488.7
HGNC ID
HGNC:6156
ChEMBL ID
CHEMBL1907598

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL78 SNV: p.K151T .
COLO792 SNV: p.S619F DBIA    Probe Info 
DU145 SNV: p.W11L .
MCC13 SNV: p.P433S DBIA    Probe Info 
NCIH1155 SNV: p.T355I; p.D653N .
NCIH661 SNV: p.V25I .
NUGC3 SNV: p.I417N .
SKMEL30 SNV: p.D135N DBIA    Probe Info 
T98G SNV: p.M213I DBIA    Probe Info 

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
OPA-S-S-alkyne
 Probe Info  		K98(1.59)  LDD3494  [1]
DBIA
 Probe Info  		C521(1.35)  LDD3310  [2]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [3]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C210(2.62)  LDD2243  [2]
 LDCM0023  KB03 22RV1 C210(4.97)  LDD2660  [2]
 LDCM0024  KB05 COLO792 C521(1.35)  LDD3310  [2]

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
Tyrosine-protein phosphatase non-receptor type 1 (PTPN1) Protein-tyrosine phosphatase family P18031
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Filamin-A (FLNA) Filamin family P21333
Integrin alpha-V (ITGAV) Integrin alpha chain family P06756
Talin-1 (TLN1) . Q9Y490
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Fractalkine (CX3CL1) Intercrine delta family P78423
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Integrin alpha-IIb (ITGA2B) Integrin alpha chain family P08514
Integrin beta-3 (ITGB3) Integrin beta chain family P05106

The Drug(s) Related To This Target

Approved
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Antithymocyte Immunoglobulin (Rabbit) BiotechDrug DB00098
Abciximab Monoclonal antibody DB00054
Eptifibatide Protein/peptide DB00063
Levothyroxine Small molecular drug DB00451
Tirofiban Small molecular drug DB00775
Ferric Cation . DB13949
Ferric Maltol . DB15598
Tetraferric Tricitrate Decahydrate . DB14520
Investigative
Click To Hide/Show 71 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 196103 Antisense drug D0Q2ZS
Isis 25237 Antisense drug D02MYZ
3-(3-(Benzamido)-5-nitrobenzamido)Propanoic Acid Small molecular drug D0G7QJ
3-(3-(Carbamoyl)Benzamido)-3-phenylpropanoic Acid Small molecular drug D0TP8S
3-(3-(Carbamoyl)Benzamido)Propanoic Acid Small molecular drug D01ZJF
Ac-asp-arg-leu-asp-ser-oh Small molecular drug D01AXA
Acdrgds Small molecular drug D0X4EE
C(-grgdfl-) Small molecular drug D0B4JU
C(Arg-gly-asp-d-phe-val) Small molecular drug D08DSG
C(Rgdff) Small molecular drug D00YBU
C(Rgdfmef) Small molecular drug D07UOF
C-[-arg-gly-asp-acpca30-] Small molecular drug D05VEC
C-[-arg-gly-asp-acpca31-] Small molecular drug D09PLA
C-[-arg-gly-asp-acpca32-] Small molecular drug D01MGI
C-[-arg-gly-asp-acpca33-] Small molecular drug D0UE7H
Cyclo(Rgdfv) (Control) Small molecular drug D0G8JI
Cyclo-[-arg-gly-asp-amp21-] Small molecular drug D03YLY
Cyclo-[-arg-gly-asp-amp22-] Small molecular drug D03KLT
Cyclo-[-arg-gly-asp-amp23-] Small molecular drug D0Z6WZ
Cyclo-[-arg-gly-asp-amp24-] Small molecular drug D0O9FL
Cyclo-[-arg-gly-asp-amp25-] Small molecular drug D07QJD
Cyclo-[-arg-gly-asp-amp26-] Small molecular drug D05GXK
Cyclo-[-arg-gly-asp-amp27-] Small molecular drug D0U0VF
Cyclo-[-arg-gly-asp-amp28-] Small molecular drug D0J6SP
Cyclorgdfv Small molecular drug D0ID6U
C[-arg-gly-asp-acpca19-] Small molecular drug D0LF7W
C[-arg-gly-asp-acpca20-] Small molecular drug D0W6CJ
C[-arg-gly-asp-acpca21-] Small molecular drug D01BZH
C[-arg-gly-asp-acpca22-] Small molecular drug D0R9GW
C[-arg-gly-asp-acpca34-] Small molecular drug D0O6DN
C[-arg-gly-asp-acpca35-] Small molecular drug D04WVG
C[-arg-gly-asp-acpca36-] Small molecular drug D06JLN
C[Rgd-(R)-alpha-tfmfv] Small molecular drug D0U2NV
C[Rgd-(S)-alpha-tfmfv] Small molecular drug D0V0JC
C[Rgdf-(R)-alpha-tfmf] Small molecular drug D0M0BN
C[Rgdf-(R)-alpha-tfmv] Small molecular drug D08CFM
C[Rgdf-(R)-n-me-alpha-tfmf] Small molecular drug D0H4EK
C[Rgdf-(S)-alpha-tfmf] Small molecular drug D0I5BY
C[Rgdf-(S)-alpha-tfmv] Small molecular drug D05EWB
C[Rgdf-(S)-n-me-alpha-tfmf] Small molecular drug D0M6NQ
C[Rgdf-(S,R)-alpha-dfm-f] Small molecular drug D0WK2F
Fradafiban Small molecular drug DB06472
Gly-arg-gly-asp-ser Small molecular drug D06LKH
Gly-arg-gly-asp-ser-pro-lys Small molecular drug D0LV6B
Isonipecotamide Small molecular drug D0H4MB
L-734115 Small molecular drug D0C8LA
L-739758 Small molecular drug D01XUU
L-746233 Small molecular drug D0S8DT
L-750034 Small molecular drug D05AGK
L-756568 Small molecular drug D06LHH
L-767679 Small molecular drug D0W5ZK
Lefradafiban Small molecular drug DB04863
N-(3,5-dichlorophenyl)Imidodicarbonimidic Diamide Small molecular drug D0R9AD
Resveratrol Small molecular drug DB02709
Roxifiban Small molecular drug D04BHL
Rwj-53419 Small molecular drug D04XTP
Sb-265123 Small molecular drug D0R3CY
Sc-54701a Small molecular drug D08RLR
St-1646 Small molecular drug D0R9SJ
Cyclo[Rgdfk(Cypate)] . D0T1II
Cypate-[(Rgd)2-nh2]1 . D0P4RB
Cypate-[(Rgd)2-nh2]2 . D04MCL
Cypate-[(Rgd)3-nh2]1 . D0L2PQ
Cypate-[(Rgd)3-nh2]2 . D0UO0Y
Cypate-[(Rgd)4-nh2]1 . D0Y8UD
Cypate-[(Rgd)4-nh2]2 . D0N9NA
E[C(Rgdyk)]2 . D05MJG
E[C(Rgdyk)]2-ptx Conjugate . D0K5DM
Lm-609 . DB05787
Rgdechi . D0D4QZ
Sb-207043 . D0M7KS
Discontinued
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dmp-757 Small molecular drug D0U4ZY
Dmp-802 Small molecular drug D0K0NP
L-709780 Small molecular drug D03GCN
L-738167 Small molecular drug D08LIG
Ro-43-5054 Small molecular drug D0Z0XQ
Ro-43-8857 Small molecular drug D03QHI
Sb-223245 Small molecular drug D0LT1S
Sc-47643 Small molecular drug D0G9BX
Skf-107260 Small molecular drug D08CQL
Xemilofiban Small molecular drug D07EXV

References

1 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
2 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
3 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