A novel class of ion displacement ligands as antagonists of the alpha IIb beta 3 receptor that limit conformational reorganization of the receptor

A novel class of ion displacement ligands as antagonists of the alpha IIb beta 3 receptor that limit conformational reorganization of the receptor

A collection of alpha IIb beta 3 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 potenti...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2014-02, Vol.24 (4), p.1148-1153
Hauptverfasser: Jiang, Jian-kang, McCoy, Joshua, Shen, Min, LeClair, Christopher, Huang, Wenwei, Negri, Ana, Li, Jihong, Blue, Robert, Harrington, Amanda, Naini, Sarasija, III, George, Choi, Won-Seok, Volpi, Elisabetta, Fernandez, Joseph, Babayeva, Mariana, Nedelman, Mark, Filizola, Marta, Coller, Barry, Thomas, Craig
Format: Artikel
Sprache:eng
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Zusammenfassung:A collection of alpha IIb beta 3 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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2013.12.122