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A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor.


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.

SUBMITTER: Jiang JK 

PROVIDER: S-EPMC3951875 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature