What question did this study set out to answer?

To investigate the pharmacological and signaling effects of the synthetic peptide ligand YFLLRNP on the human platelet thrombin receptor.

July 1, 1993Journal of Biological ChemistryOpen Access

A peptide ligand of the human thrombin receptor antagonizes alpha-thrombin and partially activates platelets

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Population

Human platelets

Design

Preclinical

Authors

URUlla RasmussenStockholm University CGChristian GachetGeneral / Preventive / Lipids YSY. SchlesingerTransgene (France)

Discussion

Member takes

Implication

Hypothesis-generating for selective thrombin receptor modulators; animal data leaves open human translation and clinical testing.

Key Points

To investigate the pharmacological and signaling effects of the synthetic peptide ligand YFLLRNP on the human platelet thrombin receptor.
Assayed human platelet aggregation induced by low concentrations of alpha-thrombin and the agonist peptide SFLLRNP in the presence of YFLLRNP.
Evaluated shape change, Ca2+ mobilization, pleckstrin (P47) phosphorylation, and secretion in platelets exposed to YFLLRNP, with and without 10 µM adrenaline prestimulation and inhibitors including prostacyclin, EDTA, aspirin, and apyrase.
YFLLRNP antagonized platelet aggregation induced by low-dose alpha-thrombin and SFLLRNP, while directly triggering pseudopod formation and potentiating responses to ADP and platelet-activating factor.
Platelets exposed to YFLLRNP exhibited no detectable Ca2+ mobilization, P47 phosphorylation, secretion, or aggregation unless prestimulated with 10 µM adrenaline in the presence of fibrinogen.
YFLLRNP-induced shape change was inhibited by prostacyclin, but remained unaffected by EDTA, aspirin, or apyrase.

Structured PICO

Population

Human platelets

Intervention

Peptide YFLLRNP

Outcome

Platelet aggregation and activation responses (shape change, Ca2+ mobilization, P47 phosphorylation, secretion)surrogate

The peptide YFLLRNP acts as a partial agonist/antagonist at the human thrombin receptor, uncoupling platelet shape change from full aggregation and secretion.

Cite This Study

Rasmussen et al. (1993) studied this question.

synapsesocial.com/papers/6a764df4329619356706dfcd https://doi.org/10.1016/s0021-9258(19)85244-4

Topics

Dual antiplatelet therapy

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A peptide ligand of the human thrombin receptor antagonizes alpha-thrombin and partially activates platelets

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

Topics

A peptide ligand of the human thrombin receptor antagonizes alpha-thrombin and partially activates platelets

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

Also Consider

Topics

Also Consider