November 14, 2012BloodOpen Access

Biased agonism of protease-activated receptor 1 by activated protein C caused by noncanonical cleavage at Arg46

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Population

Endothelial cells (in vitro) and mice (in vivo)

Design

Preclinical

Authors

LMLaurent O. MosnierScripps Research Institute RSRanjeet Kumar SinhaScripps Research Institute LBLaurent BurnierUniversity of Geneva

Discussion

Member takes

Implication

Supports biased PAR1 agonism for endothelial protection in mice; leaves open translation to human vascular therapies.

Structured PICO

Population

Endothelial cells (in vitro) and mice (in vivo)

Intervention

Activated protein C (APC) and synthetic peptide TR47 (PAR1 residues 47-66)

Outcome

PAR1 cleavage at Arg46, cytoprotective signaling (Akt and glycogen synthase kinase 3β phosphorylation, Ras-related C3 botulinum toxin substrate 1 activation, barrier stabilization), and reduction of VEGF-induced vascular leakagesurrogate

Activated protein C exerts cytoprotective effects via noncanonical cleavage of PAR1 at Arg46, generating a novel biased agonist that stabilizes endothelial barriers.

Cite This Study

Mosnier et al. (2012) studied this question.

synapsesocial.com/papers/6a7d4925469c795fc42798e9 https://doi.org/10.1182/blood-2012-08-452169

Topics

Dual antiplatelet therapy

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Biased agonism of protease-activated receptor 1 by activated protein C caused by noncanonical cleavage at Arg46

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

Biased agonism of protease-activated receptor 1 by activated protein C caused by noncanonical cleavage at Arg46

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Topics

Also Consider