Biochemical Pharmacology volume 78, issue 11, P1382-1390 2009 DOI: 10.1016/j.bcp.2009.07.007 View full text
Philip E. Boulais, Dominic Dulude, Jérôme Cabana, Nikolaus Heveker, Emanuel Escher, Pierre Lavigne, Richard Leduc

Abstract: CXCR4, a G-protein-coupled receptor, which binds the chemokine stromal cell-derived factor 1 alpha (SDF-1alpha, CXCL12), is one of two co-receptors most frequently used by HIV-1 to infect CD4+ lymphocytes. The SDF-1alpha/CXCR4 axis is also involved in angiogenesis, in stem cell homing to bone marrow, in rheumatoid arthritis and in cancer. Here, we directly determined the binding site of the inverse agonist T140 on CXCR4 using photoaffinity labeling. Two T140 photoanalogs were synthesized containing the photore…

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