title: An osteoclast-targeting agent for imaging and therapy of bone metastasis.
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.
authors.affiliation: Department of Radiology, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Boulevard, TX 75390, USA.
authors.forename: Wei
authors.initials: W
authors.lastname: Liu
authors.forename: Asghar
authors.initials: A
authors.lastname: Hajibeigi
authors.forename: Mai
authors.initials: M
authors.lastname: Lin
authors.forename: Cynthia L
authors.initials: CL
authors.lastname: Rostollan
authors.forename: Zoltan
authors.initials: Z
authors.lastname: Kovacs
authors.forename: Orhan K
authors.initials: OK
authors.lastname: Oz
authors.forename: Xiankai
authors.initials: X
authors.lastname: Sun
mesh_terms: D000818:Animals; D001859:Bone Neoplasms / Q000000981:diagnostic imaging* / Q000188:drug therapy* / Q000556:secondary; D002478:Cells, Cultured; D003952:Diagnostic Imaging; D004164:Diphosphonates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D007205:Indium Radioisotopes; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010010:Osteoclasts / Q000378:metabolism*; D011877:Radionuclide Imaging
chemical_list: C520644:1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid; D004164:Diphosphonates; D006573:Heterocyclic Compounds, 1-Ring; D007205:Indium Radioisotopes; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid