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Bioorg Med Chem Lett. 2014 Feb 15;24(4):1148-53. doi: 10.1016/j.bmcl.2013.12.122. Epub 2014 Jan 8.

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

Author information

1
NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
2
Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, NY, United States.
3
Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
4
Proteomics Resource Center, Rockefeller University, New York, NY, United States.
5
Touro College of Pharmacy, New York, NY, United States.
6
Ekam Imaging, Boston, MA, United States.
7
NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States. Electronic address: craigt@mail.nih.gov.

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.

KEYWORDS:

Ion displacement ligand; Platelet; αIIbβ3 Integrin receptor

PMID:
24461295
PMCID:
PMC3951875
DOI:
10.1016/j.bmcl.2013.12.122
[Indexed for MEDLINE]
Free PMC Article
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