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Related Experiment Videos

Receptors that activate platelets.

R W Colman1

  • 1Thrombosis Research Center, Temple University School of Medicine, Philadelphia, Pennsylvania 19140.

Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.)
|July 1, 1991
PubMed
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This review details platelet receptors, including identified receptors for ADP (aggregin), collagen (GPIa/IIa, GPIV), thromboxane A2, and alpha 2-adrenergic receptors. Understanding these receptors and their signaling pathways can lead to more targeted drug therapies.

Area of Science:

  • Biochemistry
  • Pathology
  • Cell and Molecular Biology

Background:

  • Platelet receptors play a critical role in hemostasis and thrombosis.
  • Advances in molecular biology have enabled the identification and characterization of various platelet receptors.

Purpose of the Study:

  • To review the current understanding of platelet receptor biochemistry, pathology, and molecular biology.
  • To highlight the identification and function of specific platelet receptors, including those for ADP, collagen, thromboxane A2, and thrombin.
  • To discuss the potential for developing targeted therapeutics based on a deeper knowledge of platelet receptor function and stimulus-response coupling.

Main Methods:

  • Affinity labeling (FSBA) to identify ADP receptor (aggregin).
  • Receptor antagonists and photoaffinity labeling to identify thromboxane A2 receptor.

Related Experiment Videos

  • Cloning and expression of the alpha 2-adrenergic receptor.
  • Identification of putative collagen receptors (GPIa/IIa, GPIV).
  • Tentative identification of the thrombin receptor as GPIb.

    • Main Results:

    • Aggregin (100-kDa membrane protein) identified as the ADP receptor, mediating shape change, aggregation, and fibrinogen binding site exposure.
    • Multiple collagen receptors proposed, with GPIa/IIa and GPIV as key candidates.
    • Thromboxane A2 receptor identified.
    • Alpha 2-adrenergic receptor cloned and expressed.
    • Thrombin binding to GPIb activates calpain, cleaving aggregin and exposing GPIIb/IIIa for platelet aggregation.

    Conclusions:

    • Isolation and expression of ADP, collagen, and thrombin receptors as single gene products are crucial.
    • A comprehensive understanding of stimulus-response coupling is needed.
    • This knowledge will enable the development of highly specific drugs with targeted therapeutic actions in platelet-related disorders.