Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening

Bioconjugate Chemistry
Wataru NomuraHirokazu Tamamura

Abstract

Development of CXCR4-specific ligands is an important issue in chemotherapy of HIV infection, cancer metastasis, and rheumatoid arthritis, and numerous potential ligands have been developed to date. However, it is difficult to assess their binding mode and specificity because of uncertainties in the structure of the CXCR4-ligand complexes. To address this problem, we have synthesized fluorophore labeled Ac-TZ14011, which is derived from T140, a powerful CXCR4 antagonist. Binding of Ac-TZ14011 to CXCR4 on the cell membrane was observed by fluorescence microscope, and analysis of the binding data produced IC 50 values of several ligands comparable to those obtained in RI-based assays. This fluorescence-based assay is applicable to explore new pharmacophores of CXCR4-specific ligands with high-throughput screening and also to screening of the other GPCR binding ligands.

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Citations

Apr 13, 2011·Bioconjugate Chemistry·Joeri KuilFijs W B van Leeuwen
Mar 28, 2013·Chemical Reviews·Prakasam ThirumuruganKrzysztof Jozwiak
Nov 17, 2011·Molecular Pharmaceutics·Joeri KuilFijs W B van Leeuwen
Jun 15, 2013·Nature Protocols·Alexander Emami-NeminiMartin J Lohse
Aug 12, 2014·Chemical & Pharmaceutical Bulletin·Nami OhashiHirokazu Tamamura
May 17, 2011·Current Opinion in Chemical Biology·Kelly A Daggett, Thomas P Sakmar
Jul 2, 2014·Journal of Medicinal Chemistry·Zhao MaMinyong Li
Sep 24, 2013·Biochimica Et Biophysica Acta·Rajashri SridharanMark E Dumont
Oct 27, 2010·Journal of the American Chemical Society·Tomohiro TanakaHirokazu Tamamura
Jan 13, 2017·Journal of Peptide Science : an Official Publication of the European Peptide Society·Tomohiro TanakaHirokazu Tamamura
Oct 15, 2011·Chembiochem : a European Journal of Chemical Biology·James C KnightPeter G Edwards
Oct 3, 2017·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Wataru Nomura
Apr 28, 2011·Molecular Imaging·Lucia M A CraneGooitzen M van Dam
Jun 22, 2010·Biopolymers·Wataru NomuraHirokazu Tamamura
Sep 25, 2019·Molecular Pharmacology·Ilze AdlereRob Leurs
Apr 21, 2012·Organic & Biomolecular Chemistry·Shinya Oishi, Nobutaka Fujii
Jun 30, 2012·Chemical Society Reviews·Joeri KuilFijs W B van Leeuwen
Jul 31, 2013·Biopolymers·Nami OhashiHirokazu Tamamura
Jul 9, 2011·Chembiochem : a European Journal of Chemical Biology·Joeri KuilFijs W B van Leeuwen
Aug 16, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Siyu ZhuZiwei Huang
Nov 30, 2019·Biomedical Microdevices·Yeongseok JangJonghyun Oh
Apr 12, 2019·Bioconjugate Chemistry·Maxwell M SakyiamahHirokazu Tamamura

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