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Bioorg Med Chem Lett. 2009 Dec 15;19(24):6902-6. doi: 10.1016/j.bmcl.2009.10.077. Epub 2009 Oct 22.

Identification of novel agonists of the integrin CD11b/CD18.

Author information

  • 1Peggy and Harold Katz Family Drug Discovery Center, Division of Nephrology and Hypertension, Department of Medicine and University of Miami, Miami, FL 33176, USA.

Abstract

We report the identification of novel small molecule agonists of integrin CD11b/CD18, which increased, in a dose-dependent manner, the adhesion of the integrin CD11b/CD18 expressing cells to two physiologically relevant ligands: Fibrinogen and iC3b. Compound 6 showed an ex vivo EC(50) of 10.5 microM and in vitro selectivity for binding to the recombinant alphaA-domain of CD11b/CD18. In silico docking experiments suggest that the compounds recognized a hydrophobic cleft in the ligand-binding alphaA-domain, implying an allosteric mechanism of modulation of integrin affinity by this novel compound.

PMID:
19879752
[PubMed - indexed for MEDLINE]
PMCID:
PMC2818319
Free PMC Article

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