| Literature DB >> 19879752 |
Mohd Hafeez Faridi1, Dony Maiguel, Constantinos J Barth, Darren Stoub, Ruth Day, Stephan Schürer, Vineet Gupta.
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.Entities:
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Year: 2009 PMID: 19879752 PMCID: PMC2818319 DOI: 10.1016/j.bmcl.2009.10.077
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823