Details of the Target

General Information of Target

Target ID LDTP02077
Target Name Integrin beta-2 (ITGB2)
Gene Name ITGB2
Gene ID 3689
Synonyms
CD18; MFI7; Integrin beta-2; Cell surface adhesion glycoproteins LFA-1/CR3/p150,95 subunit beta; Complement receptor C3 subunit beta; CD antigen CD18
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLGLRPPLLALVGLLSLGCVLSQECTKFKVSSCRECIESGPGCTWCQKLNFTGPGDPDSI
RCDTRPQLLMRGCAADDIMDPTSLAETQEDHNGGQKQLSPQKVTLYLRPGQAAAFNVTFR
RAKGYPIDLYYLMDLSYSMLDDLRNVKKLGGDLLRALNEITESGRIGFGSFVDKTVLPFV
NTHPDKLRNPCPNKEKECQPPFAFRHVLKLTNNSNQFQTEVGKQLISGNLDAPEGGLDAM
MQVAACPEEIGWRNVTRLLVFATDDGFHFAGDGKLGAILTPNDGRCHLEDNLYKRSNEFD
YPSVGQLAHKLAENNIQPIFAVTSRMVKTYEKLTEIIPKSAVGELSEDSSNVVHLIKNAY
NKLSSRVFLDHNALPDTLKVTYDSFCSNGVTHRNQPRGDCDGVQINVPITFQVKVTATEC
IQEQSFVIRALGFTDIVTVQVLPQCECRCRDQSRDRSLCHGKGFLECGICRCDTGYIGKN
CECQTQGRSSQELEGSCRKDNNSIICSGLGDCVCGQCLCHTSDVPGKLIYGQYCECDTIN
CERYNGQVCGGPGRGLCFCGKCRCHPGFEGSACQCERTTEGCLNPRRVECSGRGRCRCNV
CECHSGYQLPLCQECPGCPSPCGKYISCAECLKFEKGPFGKNCSAACPGLQLSNNPVKGR
TCKERDSEGCWVAYTLEQQDGMDRYLIYVDESRECVAGPNIAAIVGGTVAGIVLIGILLL
VIWKALIHLSDLREYRRFEKEKLKSQWNNDNPLFKSATTTVMNPKFAES
Target Type
Clinical trial
Target Bioclass
Other
Family
Integrin beta chain family
Subcellular location
Cell membrane
Function
Integrin ITGAL/ITGB2 is a receptor for ICAM1, ICAM2, ICAM3 and ICAM4. Integrin ITGAL/ITGB2 is also a receptor for the secreted form of ubiquitin-like protein ISG15; the interaction is mediated by ITGAL. Integrins ITGAM/ITGB2 and ITGAX/ITGB2 are receptors for the iC3b fragment of the third complement component and for fibrinogen. Integrin ITGAX/ITGB2 recognizes the sequence G-P-R in fibrinogen alpha-chain. Integrin ITGAM/ITGB2 recognizes P1 and P2 peptides of fibrinogen gamma chain. Integrin ITGAM/ITGB2 is also a receptor for factor X. Integrin ITGAD/ITGB2 is a receptor for ICAM3 and VCAM1. Contributes to natural killer cell cytotoxicity. Involved in leukocyte adhesion and transmigration of leukocytes including T-cells and neutrophils. Triggers neutrophil transmigration during lung injury through PTK2B/PYK2-mediated activation. Integrin ITGAL/ITGB2 in association with ICAM3, contributes to apoptotic neutrophil phagocytosis by macrophages. In association with alpha subunit ITGAM/CD11b, required for CD177-PRTN3-mediated activation of TNF primed neutrophils.
TTD ID
T10513
Uniprot ID
P05107
DrugMap ID
TTIJWR7
Ensemble ID
ENST00000355153.8
HGNC ID
HGNC:6155
ChEMBL ID
CHEMBL3631

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
SAA-alkyne
 Probe Info  		1.10  LDD0252  [1]
Johansson_61
 Probe Info  		_(20.00)  LDD1491  [2]
DBIA
 Probe Info  		C564(0.97); C573(0.97); C575(0.97)  LDD0078  [3]
4-Iodoacetamidophenylacetylene
 Probe Info  		C472(0.00); C286(0.00); C198(0.00); C400(0.00)  LDD0038  [4]
IA-alkyne
 Probe Info  		C472(0.00); C62(0.00); C198(0.00); C400(0.00)  LDD0036  [4]
Lodoacetamide azide
 Probe Info  		C472(0.00); C62(0.00); C286(0.00); C198(0.00)  LDD0037  [4]
Compound 10
 Probe Info  		N.A.  LDD2216  [5]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IMP2070
 Probe Info  		2.20  LDD0367  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0020  ARS-1620 HCC44 C564(0.97); C573(0.97); C575(0.97)  LDD0078  [3]
 LDCM0617  Fragment63-S Jurkat _(20.00)  LDD1491  [2]
 LDCM0022  KB02 T cell-activated C286(6.74); C575(5.05)  LDD1704  [7]
 LDCM0023  KB03 Jurkat C286(5.02)  LDD0209  [8]
 LDCM0024  KB05 IGR37 C497(1.71)  LDD3314  [9]

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 kinase ABL1 (ABL1) Tyr protein kinase family P00519
Transporter and channel
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transmembrane 4 L6 family member 18 (TM4SF18) L6 tetraspanin family Q96CE8
LHFPL tetraspan subfamily member 5 protein (LHFPL5) LHFP family Q8TAF8
Membrane-spanning 4-domains subfamily A member 7 (MS4A7) MS4A family Q9GZW8
Uroplakin-1b (UPK1B) Tetraspanin (TM4SF) family O75841
Talin-2 (TLN2) . Q9Y4G6
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Forkhead box protein D4-like 6 (FOXD4L6) . Q3SYB3
Other
Click To Hide/Show 11 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apolipoprotein L2 (APOL2) Apolipoprotein L family Q9BQE5
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
Translation initiation factor IF-3, mitochondrial (MTIF3) IF-3 family Q9H2K0
Integrin alpha-X (ITGAX) Integrin alpha chain family P20702
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Kelch-like ECH-associated protein 1 (KEAP1) KEAP1 family Q14145
Keratin-associated protein 10-8 (KRTAP10-8) KRTAP type 10 family P60410
Notch homolog 2 N-terminal-like protein A (NOTCH2NLA) NOTCH family Q7Z3S9
Notch homolog 2 N-terminal-like protein C (NOTCH2NLC) NOTCH family P0DPK4
Radixin (RDX) . P35241
Transforming growth factor-beta-induced protein ig-h3 (TGFBI) . Q15582

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rp-l201 Gene therapy DQ0I4N
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
A-286982 Small molecular drug D07XCA
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mln-2201 Antibody D07NYF
Bms-587101 . D0GT8W
Uk-279,276 . D04ZWH

References

1 Chemoproteomics and Phosphoproteomics Profiling Reveals Salvianolic Acid A as a Covalent Inhibitor of mTORC1. J Proteome Res. 2023 Jul 7;22(7):2450-2459. doi: 10.1021/acs.jproteome.3c00188. Epub 2023 Jun 22.
2 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
3 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
4 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
5 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
6 A Probe for NLRP3 Inflammasome Inhibitor MCC950 Identifies Carbonic Anhydrase 2 as a Novel Target. ACS Chem Biol. 2021 Jun 18;16(6):982-990. doi: 10.1021/acschembio.1c00218. Epub 2021 May 18.
Mass spectrometry data entry: PXD024915 , PXD024913
7 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
8 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.
9 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