An osteoclast-targeting agent for imaging and therapy of bone metastasis

Wei Liu, Asghar Hajibeigi, Mai Lin, Cynthia L. Rostollan, Zoltan Kovacs, Orhan K. Öz, Xiankai Sun

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

A hybrid compound (DO3A-BP) featuring a radiometal bifunctional chelator (1,4,7,10-tetraazacyclotetradecane-N,N′,N″,N‴-tetraac etic acid, DOTA) and an osteoclast-targeting moiety (bisphosphonate) was designed and synthesized. The 111In-labeled complex of DO3A-BP showed significantly elevated uptake in osteoclasts compared to the undifferentiated adherent bone marrow derived cells. Biodistribution studies revealed a favorable tissue distribution profile in normal mice with high bone uptake and long retention, and low or negligible accumulation in non-target organs.

Original languageEnglish (US)
Pages (from-to)4789-4793
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number17
DOIs
Publication statusPublished - Sep 1 2008

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Keywords

  • Bifunctional chelator
  • Bisphosphonate
  • Bone metastasis
  • Imaging agent
  • Indium-111
  • Osteoclast

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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