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Small molecule chemokine mimetics suggest a molecular basis for the observation that CXCL10 and CXCL11 are allosteric ligands of CXCR3
Author(s) -
Nedjai Belinda,
Li Hubert,
Stroke Ilana L,
Wise Emma L,
Webb Maria L,
Merritt J Robert,
Henderson Ian,
Klon Anthony E,
Cole Andrew G,
Horuk Richard,
Vaidehi Nagarajan,
Pease James E
Publication year - 2012
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2011.01660.x
Subject(s) - allosteric regulation , chemistry , cxcr3 , cxcl10 , small molecule , chemokine , chemokine receptor , cxcl11 , biochemistry , microbiology and biotechnology , receptor , biology
The chemokine receptor CXCR3 directs migration of T-cells in response to the ligands CXCL9/Mig, CXCL10/IP-10 and CXCL11/I-TAC. Both ligands and receptors are implicated in the pathogenesis of inflammatory disorders, including atherosclerosis and rheumatoid arthritis. Here, we describe the molecular mechanism by which two synthetic small molecule agonists activate CXCR3.