Article
Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists.
Proceedings of the National Academy of Sciences of the United States of America - 17 Nov 2020
Işbilir Ali, Möller Jan, Arimont Marta, Bobkov Vladimir, Perpiñá-Viciano Cristina, Hoffmann Carsten, Inoue Asuka, Heukers Raimond, de Graaf Chris, Smit Martine J, Annibale Paolo, Lohse Martin J
Abstract excerpt
Although class A G protein-coupled receptors (GPCRs) can function as monomers, many of them form dimers and oligomers, but the mechanisms and functional relevance of such oligomerization is ill understood. Here, we investigate this problem for the CXC chemokine receptor 4 (CXCR4), a GPCR that regulates immune and hematopoietic cell trafficking, and a major drug target in cancer therapy. We combine single-molecule...
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