Chemical subtleties in small-molecule modulation of peptide receptor function: the case of CXCR3 biaryl-type ligands

…, L Roumen, M Canals, H Custers, M Glas…

文献索引：Wijtmans, Maikel; Scholten, Danny J.; Roumen, Luc; Canals, Meritxell; Custers, Hans; Glas, Marjolein; Vreeker, Marlies C.A.; De Kanter, Frans J.J.; De Graaf, Chris; Smit, Martine J.; De Esch, Iwan J.P.; Leurs, Rob Journal of Medicinal Chemistry, 2012 , vol. 55, # 23 p. 10572 - 10583

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被引用次数: 10

摘要

The G protein-coupled chemokine receptor CXCR3 plays a role in numerous inflammatory events. The endogenous ligands for the chemokine receptors are peptides, but in this study we disclose small-molecule ligands that are able to activate CXCR3. A class of biaryl-type compounds that is assembled by convenient synthetic routes is described as a new class of CXCR3 agonists. Intriguingly, structure–activity relationship and structure–function ...