Receptor mediated uptake of a radiolabeled contrast agent sensitive to β-galactosidase activity

Mian M. Alauddin; Angelique Y. Louie; Antranik Shahinian; Thomas J. Meade; Peter S. Conti

doi:10.1016/S0969-8051(02)00392-X

Receptor mediated uptake of a radiolabeled contrast agent sensitive to β-galactosidase activity

Mian M. Alauddin, Angelique Y. Louie, Antranik Shahinian, Thomas J. Meade, Peter S. Conti

Cancer Systems Imaging

Research output: Contribution to journal › Article › peer-review

36 Scopus citations

Abstract

Radiolabeling of the MRI contrast agent 1-[2-(β-galactopyranosyloxy)propyl]-4,7,10- tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane with ¹¹¹In, and its evaluation is reported. Radiolabeling was performed in acetate buffer with 50-78% radiochemical yield. In vitro studies revealed that the asialoglycoprotein receptor-poor cell line MH1C1 has low uptake, while the receptor-rich cell lines BNL-CL2 and Hep G2 have higher uptake. In vivo, the uptake of the compound in receptor-rich organ liver was very high. Blocking the receptor in vivo, reduced liver uptake by 90% suggesting that the compound localizes in receptor-enriched tissues by binding to the asialoglycoprotein receptor.

Original language	English (US)
Pages (from-to)	261-265
Number of pages	5
Journal	Nuclear Medicine and Biology
Volume	30
Issue number	3
DOIs	https://doi.org/10.1016/S0969-8051(02)00392-X
State	Published - Apr 2003

Keywords

Asialoglycoprotein receptor
In
MRI contrast agent
β-Gal

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

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10.1016/S0969-8051(02)00392-X

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title = "Receptor mediated uptake of a radiolabeled contrast agent sensitive to β-galactosidase activity",

abstract = "Radiolabeling of the MRI contrast agent 1-[2-(β-galactopyranosyloxy)propyl]-4,7,10- tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane with 111In, and its evaluation is reported. Radiolabeling was performed in acetate buffer with 50-78% radiochemical yield. In vitro studies revealed that the asialoglycoprotein receptor-poor cell line MH1C1 has low uptake, while the receptor-rich cell lines BNL-CL2 and Hep G2 have higher uptake. In vivo, the uptake of the compound in receptor-rich organ liver was very high. Blocking the receptor in vivo, reduced liver uptake by 90% suggesting that the compound localizes in receptor-enriched tissues by binding to the asialoglycoprotein receptor.",

keywords = "Asialoglycoprotein receptor, In, MRI contrast agent, β-Gal",

author = "Alauddin, {Mian M.} and Louie, {Angelique Y.} and Antranik Shahinian and Meade, {Thomas J.} and Conti, {Peter S.}",

note = "Funding Information: The project was supported by the National Institute of General Medical Sciences grant F32 GM20526, National Institutes of Health grant AI47003-0, Biological Imaging Center of the Beckman Institute and National Institutes of Health grants: NIAID (A147003), the Human Brain Project NIMH/NIDA (DA08944) and NCRR (RR13625). ",

year = "2003",

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doi = "10.1016/S0969-8051(02)00392-X",

language = "English (US)",

volume = "30",

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AU - Alauddin, Mian M.

AU - Louie, Angelique Y.

AU - Shahinian, Antranik

AU - Meade, Thomas J.

AU - Conti, Peter S.

N1 - Funding Information: The project was supported by the National Institute of General Medical Sciences grant F32 GM20526, National Institutes of Health grant AI47003-0, Biological Imaging Center of the Beckman Institute and National Institutes of Health grants: NIAID (A147003), the Human Brain Project NIMH/NIDA (DA08944) and NCRR (RR13625).

PY - 2003/4

Y1 - 2003/4

N2 - Radiolabeling of the MRI contrast agent 1-[2-(β-galactopyranosyloxy)propyl]-4,7,10- tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane with 111In, and its evaluation is reported. Radiolabeling was performed in acetate buffer with 50-78% radiochemical yield. In vitro studies revealed that the asialoglycoprotein receptor-poor cell line MH1C1 has low uptake, while the receptor-rich cell lines BNL-CL2 and Hep G2 have higher uptake. In vivo, the uptake of the compound in receptor-rich organ liver was very high. Blocking the receptor in vivo, reduced liver uptake by 90% suggesting that the compound localizes in receptor-enriched tissues by binding to the asialoglycoprotein receptor.

AB - Radiolabeling of the MRI contrast agent 1-[2-(β-galactopyranosyloxy)propyl]-4,7,10- tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane with 111In, and its evaluation is reported. Radiolabeling was performed in acetate buffer with 50-78% radiochemical yield. In vitro studies revealed that the asialoglycoprotein receptor-poor cell line MH1C1 has low uptake, while the receptor-rich cell lines BNL-CL2 and Hep G2 have higher uptake. In vivo, the uptake of the compound in receptor-rich organ liver was very high. Blocking the receptor in vivo, reduced liver uptake by 90% suggesting that the compound localizes in receptor-enriched tissues by binding to the asialoglycoprotein receptor.

KW - Asialoglycoprotein receptor

KW - In

KW - MRI contrast agent

KW - β-Gal

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Receptor mediated uptake of a radiolabeled contrast agent sensitive to β-galactosidase activity

Abstract

Keywords

ASJC Scopus subject areas

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