Chemokine small-molecule ligands

Thiele, S., Malmgaard-Clausen, M., Engel-Andreasen, J., Steen, A., Rummel, P. C., Nielsen, M. C., et al. (2012). Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors. Journal of Medicinal Chemistry, 55, 8164-8177. 

The Binding of Small-Molecule Ligands to Chemokine Receptors... 

Kazmierski W, Bifulco N, Yang H, et al. Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors. Bioorganic Medicinal Chem 2003 11 2663-76. 

Cold (unlabeled) ligands Chemokines (Peprotech, R D systems), nanobodies, or small molecule Hgands to displace the radioligand probe. 

Chemokines are small chemotactic cytokines that act as important messenger molecules between cells of the immune system. Chemokines produce their effects by activating a family of G-protein-coupled receptors. Chemokine receptors are all seven-transmembrane glycoproteins that are structurally related. They may be characterized into those that bind to specific ligands, or those that bind several chemokine ligands. There are also virally encoded (viral) chemokine receptors that represent shared receptors that have been transduced into the viral genome during evolutionary history (Premack and SchaU 1996). 

The HIV-1 coreceptors CXCR4 and CCR5 bind to ligand members of a family of molecules known as chemokines, or chemotactic cytokines. While the hallmark function of these small proteins is the direction of leukocyte trafficking, they can also participate in cellular events such as activation and costimulation (Bajetto et al. 2(X)la). Members of the chemokine family can be classified as either homeostatic or inflammatory based on their temporal expression (Charo and Ransohoff 2006 Kim 2005). Although traditionally the CNS had been thought to be protected from immune acti-... 

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