Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells |
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| Authors: | Tanaka Tomohiro Nomura Wataru Narumi Tetsuo Masuda Akemi Tamamura Hirokazu |
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| Affiliation: | Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan. |
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| 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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