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 Citations (Scopus)

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
StatePublished - Sep 1 2008

Fingerprint

Osteoclasts
Bone
Neoplasm Metastasis
Imaging techniques
Bone and Bones
Diphosphonates
Tissue Distribution
Chelating Agents
Bone Marrow Cells
Tissue
Therapeutics
1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid

Keywords

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

ASJC Scopus subject areas

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

Cite this

An osteoclast-targeting agent for imaging and therapy of bone metastasis. / Liu, Wei; Hajibeigi, Asghar; Lin, Mai; Rostollan, Cynthia L.; Kovacs, Zoltan; Öz, Orhan K.; Sun, Xiankai.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 17, 01.09.2008, p. 4789-4793.

Research output: Contribution to journalArticle

Liu, Wei ; Hajibeigi, Asghar ; Lin, Mai ; Rostollan, Cynthia L. ; Kovacs, Zoltan ; Öz, Orhan K. ; Sun, Xiankai. / An osteoclast-targeting agent for imaging and therapy of bone metastasis. In: Bioorganic and Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 17. pp. 4789-4793.
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