doi: 10.1021/ja107447w.
Epub 2010 Oct 25.
Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells
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- PMID: 20973474
- DOI: 10.1021/ja107447w
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Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells
J Am Chem Soc.
.
Abstract
To date, challenges in the design of bivalent ligands for G protein-coupled receptors (GPCRs) have revealed difficulties stemming from lack of knowledge of the state of oligomerization of the GPCR. The synthetic bivalent ligands with rigid linkers that are presented here can predict the dimer form of CXCR4 and be applied to molecular probes in cancerous cells. This "molecular ruler" approach would be useful in elucidating the details of CXCR4 oligomer formation.
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