Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

This report describes the characterization of INCB3344, a novel, potent and selective small molecule antagonist of the mouse CCR2 receptor. The lack of rodent cross-reactivity inherent in the small molecule CCR2 antagonists discovered to date has precluded pharmacological studies of antagonists of t...

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Veröffentlicht in:	The Journal of immunology (1950) 2005-10, Vol.175 (8), p.5370-5378
Hauptverfasser:	Brodmerkel, Carrie M, Huber, Reid, Covington, Maryanne, Diamond, Sharon, Hall, Leslie, Collins, Robert, Leffet, Lynn, Gallagher, Karen, Feldman, Patricia, Collier, Paul, Stow, Mark, Gu, Xiaomei, Baribaud, Frederic, Shin, Niu, Thomas, Beth, Burn, Tim, Hollis, Greg, Yeleswaram, Swamy, Solomon, Kim, Friedman, Steve, Wang, Anlai, Xue, Chu Biao, Newton, Robert C, Scherle, Peggy, Vaddi, Kris
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arthritis, Experimental - drug therapy Cell Line Chemotaxis, Leukocyte - drug effects Chemotaxis, Leukocyte - immunology Encephalomyelitis, Autoimmune, Experimental - drug therapy Encephalomyelitis, Autoimmune, Experimental - prevention & control Female MAP Kinase Signaling System - drug effects MAP Kinase Signaling System - immunology Mice Mice, Inbred BALB C Mice, Inbred C57BL Mice, Knockout Monocytes - drug effects Protein Binding - drug effects Protein Binding - immunology Pyrrolidines - pharmacokinetics Pyrrolidines - pharmacology Rats Rats, Inbred Lew Receptors, CCR2 Receptors, Chemokine - antagonists & inhibitors Receptors, Chemokine - deficiency Receptors, Chemokine - genetics Structure-Activity Relationship
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