Overcoming challenges in developing small molecule inhibitors for GPVI and CLEC-2
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 +1 more source
ABSTRACT Platelet transfusions to treat bleeding complications use donor‐derived platelets stored at room‐temperature, that have a shelf‐life of only 5–7 days due to bacterial contamination risks. Cold‐stored and freeze‐dried platelets are being investigated for extending shelf‐life, but these still have the inherent challenge of donor‐dependency.
Ujjal Didar Singh Sekhon +20 more
wiley +1 more source
Inhibition of Glycoprotein VI Clustering by Collagen as a Mechanism of Inhibiting Collagen-Induced Platelet Responses: The Example of Losartan. [PDF]
Exposure of platelets to collagen triggers the formation of a platelet clot. Pharmacological agents capable of inhibiting platelet activation by collagen are thus of potential therapeutic interest.
Peng Jiang +5 more
doaj +1 more source
Ischemia–Reperfusion Injury: Molecular Mechanisms and Therapeutic Interventions
Multiorgan ischemia–reperfusion injury begins with ischemia‐induced ATP depletion and ionic imbalance, followed by reperfusion‐triggered mitochondrial ROS/RNS bursts, regulated cell death, and DAMP release. Sterile inflammation converges on endothelial–immune–coagulation crosstalk, where NETs drive immunothrombosis, no‐reflow, and remote organ injury ...
Peng An +4 more
wiley +1 more source
GPVI inhibition:Advancing antithrombotic therapy in cardiovascular disease [PDF]
Glycoprotein (GP) VI 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 thrombotic
Thomas, Mark R; id_orcid +2 more
core +1 more source
High-throughput elucidation of thrombus formation reveals sources of platelet function variability
In combination with microspotting, whole-blood microfluidics can provide high-throughput information on multiple platelet functions in thrombus formation.
Johanna P. van Geffen +19 more
doaj +1 more source
Model systems for platelet receptor shedding
Platelet adhesion and aggregation at sites of vascular injury are crucial for hemostasis; however, under pathological conditions, they can cause myocardial infarction and stroke.
Markus Bender +2 more
doaj +1 more source
The GPVI - Fc Fusion Protein Revacept Reduces Thrombus Formation and Improves Vascular Dysfunction in Atherosclerosis without Any Impact on Bleeding Times [PDF]
Glycoprotein VI (GPVI) is a key platelet receptor which mediates plaque-induced platelet activation and consecutive atherothrombosis, but GPVI is also involved in platelet-mediated atheroprogression.
Christine Baumgartner +15 more
core +3 more sources
Characterizing the binding site of GPVI inhibitors for the development of novel anti-platelet agents [PDF]
Ischemic cardiovascular and cerebrovascular diseases are two of the major disorders responsible for deaths and morbidity globally. Blood platelets play an important role in prevention of excessive bleeding and wound healing and their dysregulation can ...
Damaskinaki, Foteini-Nafsika
core +3 more sources
Basic mechanisms of platelet receptor shedding
Proteolytic shedding of the extracellular ectodomain of platelet receptors provides a key mechanism for irreversible loss of ligand-binding capacity, and for regulating platelet function in health and disease.
Robert K. Andrews, Elizabeth E. Gardiner
doaj +1 more source

