Targeting integrin and integrin signaling in treating thrombosis

B Estevez, B Shen, X Du - Arteriosclerosis, thrombosis, and …, 2015 - ahajournals.org
The critical roles of integrins in thrombosis have enabled the successful development and
clinical use of the first generation of integrin antagonists as represented by abciximab …

Anti-GPIIb/IIIa drugs: current strategies and future directions

BS Coller - Thrombosis and haemostasis, 2001 - thieme-connect.com
Three platelet glycoprotein (GP) IIb/IIIa receptor antagonists have been approved as
adjunctive therapy to decrease the ischemic complications of percutaneous coronary …

Acute thrombocytopenia after treatment with tirofiban or eptifibatide is associated with antibodies specific for ligand-occupied GPIIb/IIIa

DW Bougie, PR Wilker, ED Wuitschick… - Blood, The Journal …, 2002 - ashpublications.org
Acute thrombocytopenia is a recognized complication of treatment with GPIIb/IIIa inhibitors
whose cause is not yet known. We studied 9 patients who developed severe …

GPIIb/IIIa inhibitors: from bench to bedside and back to bench again

PC Armstrong, K Peter - Thrombosis and haemostasis, 2012 - thieme-connect.com
From the discovery of the platelet glycoprotein (GP) IIb/IIIa and identification of its central role
in haemostasis, the integrin GPIIb/IIIa (αIIbβ3, CD41/CD61) was destined to be an anti …

Closed headpiece of integrin αIIbβ3 and its complex with an αIIbβ3-specific antagonist that does not induce opening

J Zhu, J Zhu, A Negri, D Provasi… - Blood, The Journal …, 2010 - ashpublications.org
The platelet integrin αIIbβ3 is essential for hemostasis and thrombosis through its binding of
adhesive plasma proteins. We have determined crystal structures of the αIIbβ3 headpiece in …

Structure-Guided Design of a High-Affinity Platelet Integrin αIIbβ3 Receptor Antagonist That Disrupts Mg2+ Binding to the MIDAS

J Zhu, WS Choi, JG McCoy, A Negri, J Zhu… - Science translational …, 2012 - science.org
An integrin found on platelets, αIIbβ3 mediates platelet aggregation, and αIIbβ3 antagonists
are effective antithrombotic agents in the clinic. Ligands bind to integrins in part by …

Therapeutic expression of the platelet-specific integrin, αIIbβ3, in a murine model for Glanzmann thrombasthenia

J Fang, K Hodivala-Dilke, BD Johnson, LM Du… - Blood, 2005 - ashpublications.org
Integrins mediate the adhesion of cells to each other and to the extracellular matrix during
development, immunity, metastasis, thrombosis, and wound healing. Molecular defects in …

Intact αIIbβ3 integrin is extended after activation as measured by solution X-ray scattering and electron microscopy

ET Eng, BJ Smagghe, T Walz, TA Springer - Journal of Biological Chemistry, 2011 - jbc.org
Integrins are bidirectional signaling molecules on the cell surface that have fundamental
roles in regulating cell behavior and contribute to cell migration and adhesion …

Novel pure αVβ3 integrin antagonists that do not induce receptor extension, prime the receptor, or enhance angiogenesis at low concentrations

J Li, Y Fukase, Y Shang, W Zou… - ACS Pharmacology & …, 2019 - ACS Publications
The integrin αVβ3 receptor has been implicated in several important diseases, but no
antagonists are approved for human therapy. One possible limitation of current small …

Antibodies causing thrombocytopenia in patients treated with RGD-mimetic platelet inhibitors recognize ligand-specific conformers of αIIb3 integrin

DW Bougie, M Rasmussen, J Zhu… - Blood, The Journal of …, 2012 - ashpublications.org
Arginine-glycine-aspartic acid (RGD)–mimetic platelet inhibitors act by occupying the RGD
recognition site of αIIb/β3 integrin (GPIIb/IIIa), thereby preventing the activated integrin from …