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

doi:10.1016/j.bmcl.2008.07.092

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 journal › Article › peer-review

17 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 language	English (US)
Pages (from-to)	4789-4793
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2008.07.092
State	Published - Sep 1 2008

Keywords

Bifunctional chelator
Bisphosphonate
Bone metastasis
Imaging agent
Indium-111
Osteoclast

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2008.07.092

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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‴-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.",

keywords = "Bifunctional chelator, Bisphosphonate, Bone metastasis, Imaging agent, Indium-111, Osteoclast",

author = "Wei Liu and Asghar Hajibeigi and Mai Lin and Rostollan, {Cynthia L.} and Zoltan Kovacs and {\"O}z, {Orhan K.} and Xiankai Sun",

note = "Funding Information: This work was partially supported by an NIH R21 grant (CA119219; XS) and an unrestricted fund from the endowment of the Effie and Wofford Cain Distinguished Chair in Diagnostic Imaging provided by Dr. Robert W. Parkey. The authors like to thank Ms. Chandima Siyambalapitiyage for her assistance in the cell studies. ",

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AU - Liu, Wei

AU - Hajibeigi, Asghar

AU - Lin, Mai

AU - Rostollan, Cynthia L.

AU - Kovacs, Zoltan

AU - Öz, Orhan K.

AU - Sun, Xiankai

N1 - Funding Information: This work was partially supported by an NIH R21 grant (CA119219; XS) and an unrestricted fund from the endowment of the Effie and Wofford Cain Distinguished Chair in Diagnostic Imaging provided by Dr. Robert W. Parkey. The authors like to thank Ms. Chandima Siyambalapitiyage for her assistance in the cell studies.

PY - 2008/9/1

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N2 - 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.

AB - 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.

KW - Bifunctional chelator

KW - Bisphosphonate

KW - Bone metastasis

KW - Imaging agent

KW - Indium-111

KW - Osteoclast

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

Abstract

Keywords

ASJC Scopus subject areas

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