Discovery of a potent and orally bioavailable CCR2 and CCR5 dual antagonist

…, R Kilburn, T Wisniewski, JA DeMartino…

Index: Pasternak, Alexander; Goble, Stephen D.; Struthers, Mary; Vicario, Pasquale P.; Ayala, Julia M.; Di Salvo, Jerry; Kilburn, Ruth; Wisniewski, Thomas; Demartino, Julie A.; Mills, Sander G.; Yang, Lihu ACS Medicinal Chemistry Letters, 2010 , vol. 1, # 1 p. 14 - 18

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Citation Number: 34

Abstract

Monocyte chemoattractant protein-1 (MCP-1, CCL2), included within the CC class of chemokines,(1) mediates chemotaxis of monocytes to inflammatory sites via interactions with its receptor, CCR2.(2) CCR2, a member of the G-protein-coupled seven-transmembrane receptor superfamily, is most abundantly expressed on monocytes. The CCL2/CCR2 axis has been implicated in various autoimmune or inflammation associated diseases(3-12) including rheumatoid ...