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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

Bioconjugate chemistry

Publication Date

02/2016

Volume

27

Pages

329 - 340

Addresses

BioVinc LLC , 6162 Bristol Parkway, Culver City, California 90230, United States.

Keywords

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