PMID: 8581417Apr 1, 1995Paper

Antithrombotic agents: from RGD to peptide mimetics

Bioorganic & Medicinal Chemistry
I OjimaQ Dong

Abstract

This review covers the recent advances in the development of highly potent inhibitors of platelet aggregation as potential therapeutic drugs for thrombosis related to cardiovascular and cerebrovascular diseases. The discovery of RGD sequence-directed cell surface receptors (the integrins) has led to extensive research in the development of small RGD containing peptides and their mimetics as antithrombotic agents. These agents work by inhibiting platelet aggregation through competitive blocking of fibrinogen to the platelet surface receptor, GPIIb/IIIa. The pharmacophoric nature of the aspartic acid and arginine side chains of the RGD unit has allowed the development of strategies for rational design, largely based on assumed bioactive RGD conformations and lead optimization. Applications of such strategies, from RGD peptides to peptide hybrids and then to non-peptide mimetics, are described. Also discussed is the important issue of specificity toward GPIIb/IIIa, keeping in view that the RGD unit is a key recognition signal for a variety of cell surface receptors.

References

Mar 1, 1977·Prostaglandins·R R GormanO V Miller
Jun 1, 1978·Cell·I U Ali, R O Hynes
Nov 15, 1992·Proceedings of the National Academy of Sciences of the United States of America·D H FarrellE W Davie
Nov 13, 1992·Journal of Medicinal Chemistry·L AligT Weller
Jan 1, 1992·Seminars in Thrombosis and Hemostasis·E F PlowM H Ginsberg
Nov 27, 1992·Journal of Medicinal Chemistry·G D HartmanG Zhang
May 29, 1992·Journal of Medicinal Chemistry·P L BarkerM T Lipari
Jan 1, 1992·International Journal of Peptide and Protein Research·M J BoguskyD F Veber
Jan 31, 1992·Biochemical and Biophysical Research Communications·R MizutaniY Arata
Dec 5, 1991·European Journal of Biochemistry·C DalvitR Metternich
Dec 5, 1991·European Journal of Biochemistry·V SaudekJ T Pelton
May 1, 1991·Circulation·J H Chesebro, V Fuster
Jan 1, 1991·Annals of the New York Academy of Sciences·B S CollerD Knight
Jan 4, 1990·The New England Journal of Medicine·B S Coller
Feb 28, 1986·Cell·E Ruoslahti, M D Pierschbacher
Aug 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·E F PlowM H Ginsberg
Apr 1, 1989·Seminars in Thrombosis and Hemostasis·G DefreynJ P Maffrand
Jun 1, 1989·Proceedings of the National Academy of Sciences of the United States of America·V M GarskyP A Friedman
Oct 23, 1987·Science·E Ruoslahti, M D Pierschbacher
Dec 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·E F PlowM H Ginsberg

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Citations

Jul 2, 2008·Amino Acids·Emmanuel PapaioannouMaria Liakopoulou-Kyriakides
Sep 12, 2008·Applied Biochemistry and Biotechnology·Jintian HeHouyan Song
Dec 31, 2003·Bioorganic & Medicinal Chemistry Letters·Joanne M SmallheerPrabhakar K Jadhav
Feb 26, 2000·Enzyme and Microbial Technology·J SoB Kim
Jun 6, 2000·Advanced Drug Delivery Reviews· T Borchardt RG M Pauletti
Jul 16, 2003·Peptides·Ignacy Z Siemion, Zbigniew Wieczorek
Feb 14, 2002·European Journal of Medicinal Chemistry·Valérie GrumelGérald Guillaumet
Aug 1, 1997·Current Opinion in Biotechnology·T Kieber-EmmonsM I Greene
Mar 14, 2000·Bioorganic & Medicinal Chemistry Letters·M J FisherJ A Jakubowski
Feb 5, 2003·Bioorganic & Medicinal Chemistry Letters·Renate M van WellMark Overhand
Jan 5, 1999·Bioorganic & Medicinal Chemistry Letters·P E ThompsonM T Hearn
Nov 5, 1998·Bioorganic & Medicinal Chemistry·T BoxusJ Marchand-Brynaert
Apr 3, 2004·Nature Reviews. Drug Discovery·Michelle R Arkin, James A Wells
Jul 29, 1999·The Journal of Peptide Research : Official Journal of the American Peptide Society·S J Bogdanowich-KnippT J Siahaan
Jul 29, 1999·The Journal of Peptide Research : Official Journal of the American Peptide Society·S J Bogdanowich-KnippT J Siahaan
Sep 1, 2005·Journal of Thrombosis and Haemostasis : JTH·A KoukiD C Tsoukatos
Jul 2, 2015·Future Medicinal Chemistry·Zhouling XieZhiyu Li
Feb 24, 2001·Clinical and Applied Thrombosis/hemostasis : Official Journal of the International Academy of Clinical and Applied Thrombosis/Hemostasis·M K Orcullo SantillanJ Fareed
Sep 5, 2001·The Journal of Peptide Research : Official Journal of the American Peptide Society·J P ShannonR S Larson
Aug 26, 1998·The Journal of Peptide Research : Official Journal of the American Peptide Society·E Harth-FritschyD Cantacuzène
Jul 22, 2006·Molecular and Cellular Biochemistry·Jianbo YangJie Yang
Jul 19, 2002·Analytical Biochemistry·Paul H WeinrebSerene Josiah
Aug 2, 1996·Journal of Medicinal Chemistry·T WellerB Steiner
Jan 12, 2005·European Journal of Medicinal Chemistry·Marko AnderluhMarija Sollner Dolenc
Jan 3, 1997·Journal of Medicinal Chemistry·J WityakR E Olson
Feb 1, 2011·Journal of Medicinal Chemistry·Phuc Ung, David A Winkler
Apr 2, 2004·Journal of Medicinal Chemistry·Mukund M MehrotraRobert M Scarborough

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