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, 20 (2), 662-4

Identification of a New Class of Small Molecule C5a Receptor Antagonists

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Identification of a New Class of Small Molecule C5a Receptor Antagonists

Jack J Chen et al. Bioorg Med Chem Lett.

Abstract

C5a is a terminal product of the complement cascade that activates and attracts inflammatory cells including granulocytes, mast cells and macrophages via a specific GPCR, the C5a receptor (C5aR). Inhibition of C5a/C5aR interaction has been shown to be efficacious in several animal models of autoimmune diseases, including RA, SLE and asthma. This account reports the discovery of a new class of C5aR antagonists through high-throughput screening. The lead compounds in this series are selective and block C5a binding, C5a-promoted calcium flux in human neutrophils with nanomolar potency.

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