Fluorescent Bisphosphonate and Carboxyphosphonate Probes: A Versatile Imaging Toolkit for Applications in Bone Biology and Biomedicine

Bioconjug Chem. 2016 Feb 17;27(2):329-40. doi: 10.1021/acs.bioconjchem.5b00369. Epub 2015 Dec 8.

Abstract

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bone Diseases / diagnosis*
  • Bone and Bones / pathology*
  • Cell Line
  • Diphosphonates / chemistry*
  • Fluorescent Dyes / chemistry*
  • Humans
  • Male
  • Optical Imaging / methods*
  • Rats, Sprague-Dawley

Substances

  • Diphosphonates
  • Fluorescent Dyes