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Related Concept Videos

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Formation of the Platelet Plug01:22

Formation of the Platelet Plug

The platelet phase, the second stage of hemostasis, commences around 15-20 seconds after an injury. It follows and overlaps with the vascular phase, during which blood vessels constrict to minimize blood loss.
As the injured blood vessel contracts, endothelial cells undergo contraction, revealing collagen fibers in the basement membrane and underlying connective tissue. Furthermore, the plasma membrane of endothelial cells becomes adhesive, preparing the site for platelet adhesion. Platelets...
Structure and Function of Platelets01:18

Structure and Function of Platelets

The cell fragments known as platelets are disc-shaped, with an average diameter of about 3 μm and a thickness of roughly 1 μm. They play a crucial role in the body's vascular clotting system, which also involves plasma proteins, blood cells, and blood vessel tissues.
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IP3/DAG Signaling Pathway01:11

IP3/DAG Signaling Pathway

Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the  phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and produces two-second...
Amplifying Signals via Second Messengers01:15

Amplifying Signals via Second Messengers

Many receptor binding ligands are hydrophilic; they do not cross the cell membrane but bind to cell-surface receptors. Thus, their message must be relayed by second messengers present in the cell cytoplasm. There are several second messenger pathways, each with its own way of relaying information. For example, the G protein-coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol pathway is active when the receptor induces...
Phosphoinositides and PIPs01:42

Phosphoinositides and PIPs

Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...

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A Uniform Shear Assay for Human Platelet and Cell Surface Receptors via Cone-plate Viscometry
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Published on: June 5, 2019

P2Y12 receptor in platelet activation.

Soochong Kim1, Satya P Kunapuli

  • 1Department of Physiology, Temple University School of Medicine, Philadelphia, PA, USA.

Platelets
|January 15, 2011
PubMed
Summary

Adenosine diphosphate (ADP) is crucial for blood clotting and clot formation. Targeting the P2Y12 receptor, which ADP activates, is an effective strategy for developing antithrombotic drugs.

Area of Science:

  • Biochemistry
  • Hematology
  • Pharmacology

Background:

  • Adenosine diphosphate (ADP) is a key signaling molecule in hemostasis and thrombosis.
  • Platelet activation and aggregation are critical processes in thrombus formation.
  • The P2Y12 receptor is a primary mediator of ADP-induced platelet responses.

Purpose of the Study:

  • To highlight the significance of ADP in hemostasis and thrombosis.
  • To emphasize the central role of the P2Y12 receptor in platelet activation.
  • To underscore the therapeutic potential of targeting the P2Y12 receptor for antithrombotic drug development.

Main Methods:

  • Review of existing literature on ADP signaling in platelets.
  • Analysis of the P2Y12 receptor's function in thrombus formation.

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  • Evaluation of P2Y12 receptor antagonists as antithrombotic agents.
  • Main Results:

    • ADP is essential for normal hemostatic plug formation.
    • P2Y12 receptor activation by ADP leads to sustained platelet aggregation.
    • P2Y12 receptor blockade effectively inhibits thrombus development.

    Conclusions:

    • The P2Y12 receptor is a validated and critical target for antithrombotic therapy.
    • Understanding ADP-P2Y12 interactions provides a basis for novel antithrombotic drug design.
    • Targeting P2Y12 offers a promising approach to prevent thrombotic events.