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We report synthesis of the first fluorescently labeled conjugates of risedronate (1), using an epoxide linker strategy enabling conjugation of 1 via its pyridyl nitrogen with the label (carboxyfluorescein). Unlike prior approaches to create fluorescent bisphosphonate probes, the new linking chemistry did not abolish the ability to inhibit protein prenylation in vitro, while significantly retaining hydroxyapatite affinity. The utility of a fluorescent 1 conjugate in visualizing osteoclast resorption in vitro was demonstrated.

Original publication

DOI

10.1021/bc800369c

Type

Journal article

Journal

Bioconjugate chemistry

Publication Date

12/2008

Volume

19

Pages

2308 - 2310

Addresses

Department of Chemistry, University of Southern California, Los Angeles, California 90089-0744, USA.

Keywords

Osteoclasts, Animals, Rabbits, Etidronic Acid, Fluorescent Dyes, Magnetic Resonance Spectroscopy, Temperature