Bioorg Med Chem Lett. 2008 Sep 1;18(17):4789-93. Epub 2008 Jul 27.

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

Liu W, Hajibeigi A, Lin M, Rostollan CL, Kovacs Z, Oz OK, Sun X.

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Department of Radiology, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Boulevard, TX 75390, USA.

Abstract

A hybrid compound (DO3A-BP) featuring a radiometal bifunctional chelator (1,4,7,10-tetraazacyclotetradecane-N,N',N'',N'''-tetraacetic acid, DOTA) and an osteoclast-targeting moiety (bisphosphonate) was designed and synthesized. The (111)In-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.

PMID:: 18692394; [PubMed - indexed for MEDLINE]
PMCID:: PMC2553272

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