integrin αIIbβ3 | Integrins | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

integrin αIIbβ3

Target not currently curated in GtoImmuPdb

Target id: 2579

Nomenclature: integrin αIIbβ3

Family: Integrins

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

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
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

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
G4120 Hs Inhibition 8.4 pKi 3,6
pKi 8.4 (Ki 4x10-9 M) [3,6]
tirofiban 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 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 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 Hs Binding - - 1
[1]

References

Show »

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]

How to cite this page

Integrins: integrin αIIbβ3. Last modified on 20/10/2015. Accessed on 16/06/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2579.