Overcoming challenges in developing small molecule inhibitors for GPVI and CLEC-2
Platelets, 2021 GPVI and CLEC-2 have emerged as promising targets for long-term prevention of both arterial thrombosis and thrombo-inflammation with a decreased bleeding risk relative to current drugs.
Foteini-Nafsika Damaskinaki +4 more
doaj +2 more sources
Affimer reagents as tool molecules to modulate platelet GPVI-ligand interactions and specifically bind GPVI dimer [PDF]
Blood AdvancesKey Points • We generated Affimers against platelet GPVI and mapped their binding sites, revealing functional regions regulating ligand binding.• A dimeric epitope was identified on GPVI for Affimer D18, which specifically binds GPVI dimer through a 1:1 ...
Ruigang Xu +15 more
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Functional significance of the platelet immune receptors GPVI and CLEC-2 [PDF]
Journal of Clinical Investigation, 2019 Although platelets are best known for their role in hemostasis, they are also crucial in development, host defense, inflammation, and tissue repair. Many of these roles are regulated by the immune-like receptors glycoprotein VI (GPVI) and C-type lectin ...
Julie Rayes +2 more
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GPVI and collagen: the final word? [PDF]
Blood, 2022 Alexandre Slater +1 more
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GPIIb/IIIa-GPVI–commanded platelet patrol [PDF]
Blood, 2022 Madhumita Chatterjee
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The Platelet Collagen Receptor GPVI Is Cleaved by Tspan15/ADAM10 and Tspan33/ADAM10 Molecular Scissors [PDF]
International Journal of Molecular Sciences, 2022 The platelet-activating collagen receptor GPVI represents the focus of clinical trials as an antiplatelet target for arterial thrombosis, and soluble GPVI is a plasma biomarker for several human diseases.
Chek Ziu Koo +7 more
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GPVI inhibition: Advancing antithrombotic therapy in cardiovascular disease [PDF]
European Heart Journal - Cardiovascular PharmacotherapyGlycoprotein (GP) VI (GPVI) plays a major role in thrombosis but not haemostasis, making it a promising antithrombotic target. The primary role of GPVI on the surface of platelets is a signalling receptor for collagen, which is one of the most potent ...
Alexandre Slater +2 more
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Targeting platelet GPVI with glenzocimab: a novel mechanism for inhibition [PDF]
Blood Advances, 2022 Key Points • Crystallization studies map the binding of glenzocimab to the site of dimerization in the D2 domain of GPVI.• Glenzocimab inhibits GPVI interactions with CRP, collagen, and fibrin by loss of dimerization, conformational changes, and steric ...
Philippe Billiald +12 more
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Inhibition of platelet GPVI induces intratumor hemorrhage and increases efficacy of chemotherapy in mice [PDF]
Blood, 2019 Maintenance of tumor vasculature integrity is indispensable for tumor growth and thus affects tumor progression. Previous studies have identified platelets as major regulators of tumor vascular integrity, as their depletion selectively rendered tumor ...
Julia Volz +10 more
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Phosphoproteomic quantitation and causal analysis reveal pathways in GPVI/ITAM-mediated platelet activation programs [PDF]
Blood, 2020 Platelets engage cues of pending vascular injury through coordinated adhesion, secretion and aggregation responses. These rapid, progressive changes in platelet form and function are orchestrated downstream of specific receptors on the platelet cell ...
Özgün Babur +16 more
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