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A bone imaging toolkit of 21 fluorescent probes with variable spectroscopic properties, bone mineral binding affinities, and antiprenylation activities has been created, including a novel linking strategy. The linking chemistry allows attachment of a diverse selection of dyes fluorescent in the visible to near-infrared range to any of the three clinically important heterocyclic bisphosphonate bone drugs (risedronate, zoledronate, and minodronate or their analogues). The resultant suite of conjugates offers multiple options to "mix and match" parent drug structure, fluorescence emission wavelength, relative bone affinity, and presence or absence of antiprenylation activity, for bone-related imaging applications.

Original publication

DOI

10.1021/acs.bioconjchem.5b00369

Type

Journal article

Journal

Bioconjug Chem

Publication Date

17/02/2016

Volume

27

Pages

329 - 340

Keywords

Animals, Bone Diseases, Bone and Bones, Cell Line, Diphosphonates, Fluorescent Dyes, Humans, Male, Optical Imaging, Rats, Sprague-Dawley