June 1, 1993Journal of Medicinal Chemistry

Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Arg-guanidine of RGDX mimetics and the platelet GP IIb-IIIa receptor

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Why the study?

Does SC-52012, a peptide mimetic of the RGDF sequence, potently inhibit platelet aggregation in preclinical models?

Population

In vitro models and in vivo dog model for ex vivo collagen-induced platelet aggregation

Comparison

SC-52012 (peptide mimetic of RGDF sequence with… vs Natural RGDF ligand, benzylamine derivative, and…

Design

Preclinical

Authors

JZJeffery A. ZablockiCarolina Veterinary Specialists MMMasateru MiyanoShowa University RGRobert B. GarlandBiogen (United States)

Discussion

Member takes

Implication

High-potency platelet inhibition in dogs supports RGDF mimetic advancement; leaves open clinical translation and safety in humans.

Structured PICO

Does SC-52012, a peptide mimetic of the RGDF sequence, potently inhibit platelet aggregation in preclinical models?

Population

In vitro models and in vivo dog model for ex vivo collagen-induced platelet aggregation

Intervention

SC-52012 (peptide mimetic of RGDF sequence with 5-(4-amidinophenyl)pentanoyl replacement) administered via IV infusion

Comparator

Natural RGDF ligand, benzylamine derivative (18), and imidazoline derivative (19)

Outcome

Inhibition of platelet aggregation (ED50)surrogate

Peptide mimetics of the RGDF sequence with benzamidine replacement demonstrate potent inhibition of platelet aggregation via the GP IIb-IIIa receptor in preclinical models.

Cite This Study

Zablocki et al. (1993) studied this question.

synapsesocial.com/papers/6a8519a95c0b46d4e2991a8d https://doi.org/10.1021/jm00065a003

Topics

Dual antiplatelet therapy

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Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Arg-guanidine of RGDX mimetics and the platelet GP IIb-IIIa receptor

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Arg-guanidine of RGDX mimetics and the platelet GP IIb-IIIa receptor

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Topics

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