A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor.
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ABSTRACT:
SUBMITTER: Jiang JK
PROVIDER: S-EPMC3951875 | biostudies-literature | 2014 Feb
REPOSITORIES: biostudies-literature
Publications
A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor.
Jiang Jian-kang JK McCoy Joshua G JG Shen Min M LeClair Christopher A CA Huang Wenwei W Negri Ana A Li Jihong J Blue Robert R Harrington Amanda Weil AW Naini Sarasija S David George G Choi Won-Seok WS Volpi Elisabetta E Fernandez Joseph J Babayeva Mariana M Nedelman Mark A MA Filizola Marta M Coller Barry S BS Thomas Craig J CJ
Bioorganic & medicinal chemistry letters 20140108 4
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. ...[more]
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