A novel class of ion displacement ligands as antagonists of the αiIbβ3 receptor that limit conformational reorganization of the receptor

Jian Kang Jiang, Joshua G. McCoy, Min Shen, Christopher A. LeClair, Wenwei Huang, Ana Negri, Jihong Li, Robert Blue, Amanda Weil Harrington, Sarasija Naini, George David, Won Seok Choi, Elisabetta Volpi, Joseph Fernandez, Mariana Babayeva, Mark A. Nedelman, Marta Filizola, Barry S. Coller, Craig J. Thomas

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

A collection of αIIbβ3 integrin receptor antagonists possessing a unique MIDAS metal ion displacement mechanism of action is presented. Insight into these agents' structure-activity relationships, binding modality, and pharmacokinetic and pharmacodynamic profiles highlight the potential of these small molecule ion displacement ligands as attractive candidates for clinical development.

Original languageEnglish
Pages (from-to)1148-1153
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number4
DOIs
StatePublished - 15 Feb 2014

Keywords

  • Ion displacement ligand
  • Platelet
  • αIIbβ3 Integrin receptor

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