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Elsevier, Bioorganic and Medicinal Chemistry Letters, 24(19), p. 6902-6906

DOI: 10.1016/j.bmcl.2009.10.077

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Identification of novel agonists of the integrin CD11b/CD18

Journal article published in 2009 by Mohd Hafeez Faridi, Dony Maiguel, Constantinos J. Barth, Darren Stoub, Ruth Day, Stephan Schürer, Vineet Gupta ORCID
This paper is available in a repository.
This paper is available in a repository.

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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.