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integrin αIIbβ3

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Target not currently curated in GtoImmuPdb

Target id: 2579

Nomenclature: integrin αIIbβ3

Family: Integrins

Quaternary Structure: Subunits
integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41)
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)
Previous and Unofficial Names Click here for help
α2bβ3 | fibrinogen receptor | platelet GpIIbIIIa
Ligands (Human)
fibrinogen (FGA, FGB, FGG, P02671, P02679, P02675), fibronectin (FN1, P02751), von Willebrand factor (VWF, P04275), vitronectin (VTN, P04004), thrombospondin

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
G4120 Peptide Hs Inhibition 8.4 pKi 3,6
pKi 8.4 (Ki 4x10-9 M) [3,6]
tirofiban Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.4 pIC50 5
pIC50 9.4 (IC50 3.7x10-10 M) [5]
Description: Displacement of biotinylated fibrinogen from human integrin αIIbβ3.
GR 144053 Small molecule or natural product Hs Inhibition 7.4 pIC50 2
pIC50 7.4 (IC50 3.7x10-8 M) [2]
Description: Inhibition of ADP (10 µM)-induced aggregation in human gel-filtered platelets.
eptifibatide Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 6.2 – 6.8 pIC50 4
pIC50 6.2 – 6.8 (IC50 5.7x10-7 – 1.4x10-7 M) [4]
Description: inhibition of human platelet aggregation. The IC50 varies according to the anti-coagulant used during blood collection.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
abciximab Peptide Approved drug Primary target of this compound Hs Binding - - 1
[1]

References

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1. Coller BS, Knight DM. (1999) Method of antithrombotic therapy using anti-GPIIb/IIIa antibodies or fragments thereof, including c7E3. Patent number: US5976532. Assignee: Centocor, Inc.. Priority date: 18/05/1988. Publication date: 02/11/1999.

2. Eldred CD, Evans B, Hindley S, Judkins BD, Kelly HA, Kitchin J, Lumley P, Porter B, Ross BC, Smith KJ et al.. (1994) Orally active non-peptide fibrinogen receptor (GpIIb/IIIa) antagonists: identification of 4-[4-[4-(aminoiminomethyl)phenyl]-1-piperazinyl]-1-piperidineacetic acid as a long-acting, broad-spectrum antithrombotic agent. J Med Chem, 37 (23): 3882-5. [PMID:7966149]

3. Matsuno H, Stassen JM, Vermylen J, Deckmyn H. (1994) Inhibition of integrin function by a cyclic RGD-containing peptide prevents neointima formation. Circulation, 90 (5): 2203-6. [PMID:7955174]

4. Scarborough RM, Gretler DD. (2000) Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. J Med Chem, 43 (19): 3453-73. [PMID:10999999]

5. Trstenjak U, Ilaš J, Kikelj D. (2013) Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores. Eur J Med Chem, 64: 302-13. [PMID:23644213]

6. Yasuda T, Gold HK, Kohmura C, Guerrero L, Yaoita H, Fallon JT, Bunting S, Collen D. (1993) Intravenous and endobronchial administration of G4120, a cyclic Arg-Gly-Asp-containing platelet GPIIb/IIIa receptor-blocking pentapeptide, enhances and sustains coronary arterial thrombolysis with rt-PA in a canine preparation. Arterioscler Thromb, 13 (5): 738-47. [PMID:8485125]

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