Design, synthesis and SAR of RGD peptide hybrids as highly efficient inhibitors of platelet aggregation

@article{Ojima1995DesignSA,
  title={Design, synthesis and SAR of RGD peptide hybrids as highly efficient inhibitors of platelet aggregation},
  author={Iwao Ojima and Qing Dong and Subrata Chakravarty and Ellinor I. Peerschke and Shing Mei Hwang and Angela S. Wong},
  journal={Bioorganic \& Medicinal Chemistry Letters},
  year={1995},
  volume={5},
  pages={1941-1946}
}
  • I. Ojima, Q. Dong, A. Wong
  • Published 7 September 1995
  • Biology, Chemistry
  • Bioorganic & Medicinal Chemistry Letters
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8 Citations

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Development of the new potent non-peptide gpIIb/IIIa antagonist NSL-95301 by utilizing combinatorial technique
Design and Synthesis of RGD Mimetics as Potent Inhibitors of Platelet Aggregation
TLDR
Through a process of rational design, mimetics of the RGD sequence were synthesized, providing deeper insight into the structural requirements for high inhibitory activity, and these mimetics were found to be extremely potent inhibitors of platelet aggregation.
A Constrained Diketopiperazine as a New Scaffold for the Synthesis of Peptidomimetics
TLDR
The synthesis of new peptidomimetics of the Arg-Gly-Asp (RGD) sequence is described, which shows a selective platelet-aggregation inhibiting activity and can be used as a lead for the preparation of more potent products.
Design, Virtual Screening, and Synthesis of Antagonists of αIIbβ3 as Antiplatelet Agents.
TLDR
Design, virtual screening, synthesis, and biological tests of novel αIIbβ3 antagonists, which inhibit platelet aggregation are described, which showed that two designed ligands for the open form 4c and 4d were more potent than commercial antithrombotic Tirofiban.
Computer-aided design of novel antithrombotic agents
TLDR
The computer-aided design of new anti-thrombotic agents able to inhibit two types of receptors located on the surface of the platelets to suggest new potential antagonists of αIIbβ3 and thromboxane A2 receptors.
Molecular dynamics study of disulfide bond influence on properties of an RGD peptide.
  • Y. Wang, S. Goh, K. Kuczera
  • Chemistry, Biology
    The journal of peptide research : official journal of the American Peptide Society
  • 1999
TLDR
Three 1 ns length molecular dynamics simulations of an RGD peptide (Ac-Pen-Arg-Gly-Asp-Cys-NH2, with Pen denoting penicillamine) have been performed in aqueous solution to calculate several properties and to identify conformations explored by the two forms and to describe the physical role of the disulfide bond.
Derives d'indole servant d'antagoniste de somatostatine
L'invention concerne un compose represente par la formule (I), dans laquelle le noyau A represente un noyau aromatique possedant eventuellement des substituants ; B, Y et Ya sont semblables ou…
Engineering RGD-modified liposomes for targeted drug delivery to activated platelets.

References

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TLDR
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The tetrapeptide H-Arg-Gly-Asp-Ser-OH (1) (RGDS), representing a recognition sequence of fibrinogen for its platelet receptor GP IIb-IIIa (integrin alpha IIb beta 3), served as lead compound for the…
Cell attachment activity of fibronectin can be duplicated by small synthetic fragments of the molecule
The ability of fibronectin to bind cells can be accounted for by the tetrapeptide L-arginyl-glycyl-L-aspartyl-L-serine, a sequence which is part of the cell attachment domain of fibronectin and…
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