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Literature DB >> 18692394

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

Wei Liu¹, Asghar Hajibeigi, Mai Lin, Cynthia L Rostollan, Zoltan Kovacs, Orhan K Oz, Xiankai Sun.

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.

Entities: Chemical Disease Gene Species

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Year: 2008 PMID： 18692394 PMCID： PMC2553272 DOI： 10.1016/j.bmcl.2008.07.092

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

32 in total

1. Identification and characterization of the new osteoclast progenitor with macrophage phenotypes being able to differentiate into mature osteoclasts.

Authors: S Takeshita; K Kaji; A Kudo
Journal: J Bone Miner Res Date: 2000-08 Impact factor: 6.741

2. Comparison of yttrium and indium complexes of DOTA-BA and DOTA-MBA: models for (90)Y- and (111)In-labeled DOTA-biomolecule conjugates.

Authors: Shuang Liu; John Pietryka; Charles E Ellars; D Scott Edwards
Journal: Bioconjug Chem Date: 2002 Jul-Aug Impact factor: 4.774

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

1. Identification and characterization of the new osteoclast progenitor with macrophage phenotypes being able to differentiate into mature osteoclasts.

2. Comparison of yttrium and indium complexes of DOTA-BA and DOTA-MBA: models for (90)Y- and (111)In-labeled DOTA-biomolecule conjugates.

3. Bisphosphonate action. Alendronate localization in rat bone and effects on osteoclast ultrastructure.

4. Skull base involvement by a nasopharyngeal carcinoma shown by Tc-99m MDP SPECT but not by computed tomography.

5. The ultrastructure of the osteoclast and its functional implications.

6. Novel synthesis of bis(phosphonic acid)-steroid conjugates.

Review 7. Current and future directions in medical therapy: hypercalcemia.

Review 8. In vitro and in vivo antitumor effects of bisphosphonates.

9. Uptake and biodistribution of technetium-99m-MD32P during rat tibial bone repair.

Review 10. Diagnosis of occult bone metastases: positron emission tomography.

1. On the Synthesis of 1,4,7-Tris(tert-butoxycarbonylmethyl)-1,4,7,10-tetraazacyclododecane.

2. A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P.

3. Targeting the alphavbeta3 integrin for small-animal PET/CT of osteolytic bone metastases.