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Updated: Apr 7, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Progress in the research of GPIIb/IIIa antagonists
Zhouling Xie1, Chen Cao1, Sen Feng1
1Jiangsu key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing 210009, China.
Abstract:
This review covers the recent advances in the development of small RGD (Arg-Gly-Asp sequence) containing peptides and their mimetics as potential antithrombotic agents. Glycoprotein IIb/IIIa (GPIIb/IIIa) antagonists include monoclonal antibodies, RGD peptides, peptide hybrids and nonpeptide mimetics. The current trend in the development of nonpeptide mimetics is clearly directed toward orally active and safe antithrombotic drug candidates. But several nonpeptide mimetics, being evaluated for their oral activity in human clinical trials, are currently not approved for clinical use due to poor safety profile. It is expected that newer and more effective nonpeptide mimetics will be developed in the near future.
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