Target General Infomation
Target ID
T10513
Former ID
TTDR01170
Target Name
Integrin beta-2
Gene Name
ITGB2
Synonyms
CD18; Cell surface adhesion glycoproteins LFA-1/CR3/p150,95 subunit beta; Complement receptor C3 subunit beta; Integrin alpha-M/beta-2; ITGB2
Target Type
Discontinued
Disease Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Stroke [ICD9: 434.91, 437.6, 453, 671.5, 671.9; ICD10: I61-I63, I80-I82]
Function
Integrin alpha-L/beta-2 is a receptor for ICAM1, ICAM2, ICAM3 and ICAM4. Integrins alpha-M/beta-2 and alpha-X/beta-2 are receptors for the iC3b fragment of the third complement component and for fibrinogen. Integrin alpha-X/beta-2 recognizes thesequence G-P-R in fibrinogen alpha-chain. Integrin alpha-M/beta-2 recognizes P1 and P2 peptides of fibrinogen gamma chain. Integrin alpha-M/beta-2 is also a receptor for factor X. Integrin alpha- D/beta-2 is a receptor for ICAM3 and VCAM1. Triggers neutrophil transmigration during lung injury through PTK2B/PYK2-mediated activation.
BioChemical Class
Integrin
Target Validation
T10513
UniProt ID
Sequence
MLGLRPPLLALVGLLSLGCVLSQECTKFKVSSCRECIESGPGCTWCQKLNFTGPGDPDSI
RCDTRPQLLMRGCAADDIMDPTSLAETQEDHNGGQKQLSPQKVTLYLRPGQAAAFNVTFR
RAKGYPIDLYYLMDLSYSMLDDLRNVKKLGGDLLRALNEITESGRIGFGSFVDKTVLPFV
NTHPDKLRNPCPNKEKECQPPFAFRHVLKLTNNSNQFQTEVGKQLISGNLDAPEGGLDAM
MQVAACPEEIGWRNVTRLLVFATDDGFHFAGDGKLGAILTPNDGRCHLEDNLYKRSNEFD
YPSVGQLAHKLAENNIQPIFAVTSRMVKTYEKLTEIIPKSAVGELSEDSSNVVQLIKNAY
NKLSSRVFLDHNALPDTLKVTYDSFCSNGVTHRNQPRGDCDGVQINVPITFQVKVTATEC
IQEQSFVIRALGFTDIVTVQVLPQCECRCRDQSRDRSLCHGKGFLECGICRCDTGYIGKN
CECQTQGRSSQELEGSCRKDNNSIICSGLGDCVCGQCLCHTSDVPGKLIYGQYCECDTIN
CERYNGQVCGGPGRGLCFCGKCRCHPGFEGSACQCERTTEGCLNPRRVECSGRGRCRCNV
CECHSGYQLPLCQECPGCPSPCGKYISCAECLKFEKGPFGKNCSAACPGLQLSNNPVKGR
TCKERDSEGCWVAYTLEQQDGMDRYLIYVDESRECVAGPNIAAIVGGTVAGIVLIGILLL
VIWKALIHLSDLREYRRFEKEKLKSQWNNDNPLFKSATTTVMNPKFAES
Structure
1A8X; 1BHO; 1BHQ; 1IDN; 1IDO; 1JLM; 1M1U; 1MF7; 1N9Z; 1NA5; 2LKE; 2LKJ; 3Q3G; 3QA3; 4M76; 1JX3; 1L3Y; 1YUK; 2JF1; 2P26; 2P28; 2V7D; 3K6S; 3K71; 3K72; 4NEH; 4NEN
Drugs and Mode of Action
Drug(s) UK-279,276 Drug Info Discontinued in Phase 2 Stroke [545570]
MLN-2201 Drug Info Discontinued in Phase 1 Cerebrovascular ischaemia [546763]
Inhibitor A-286982 Drug Info [526034]
BMS-587101 Drug Info [528539]
Antagonist UK-279,276 Drug Info [536373]
Pathways
KEGG Pathway Rap1 signaling pathway
Phagosome
Hippo signaling pathway
Cell adhesion molecules (CAMs)
Natural killer cell mediated cytotoxicity
Leukocyte transendothelial migration
Regulation of actin cytoskeleton
Pertussis
Legionellosis
Leishmaniasis
Malaria
Amoebiasis
Staphylococcus aureus infection
Tuberculosis
HTLV-I infection
Rheumatoid arthritis
Viral myocarditis
NetPath Pathway IL5 Signaling Pathway
TCR Signaling Pathway
IL2 Signaling Pathway
PANTHER Pathway Integrin signalling pathway
Pathway Interaction Database Integrin family cell surface interactions
amb2 Integrin signaling
Beta2 integrin cell surface interactions
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
CXCR3-mediated signaling events
HIF-1-alpha transcription factor network
Reactome Toll Like Receptor 4 (TLR4) Cascade
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
Cell surface interactions at the vascular wall
Integrin cell surface interactions
WikiPathways Focal Adhesion
Human Complement System
Toll-Like Receptors Cascades
Integrin-mediated Cell Adhesion
Integrin cell surface interactions
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
Cell surface interactions at the vascular wall
References
Ref 545570Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003726)
Ref 546763Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010178)
Ref 526034J Med Chem. 2001 Apr 12;44(8):1202-10.Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.
Ref 528539J Med Chem. 2006 Nov 30;49(24):6946-9.Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.
Ref 536373Advances in ischemic stroke treatment: neuroprotective and combination therapies. Expert Opin Emerg Drugs. 2007 Mar;12(1):97-112.
Ref 546764Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010178)

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