Gadolinium complex of 125I/127I-RGD-DOTA conjugate as a tumor-targeting SPECT/MR bimodal imaging probe

Ji Ae Park; Jung Young Kim; Yong Jin Lee; Wonho Lee; Sang Moo Lim; Tae Jeong Kim; Jeongsoo Yoo; Yongmin Chang; Kyeong Min Kim

doi:10.1021/ml3003499

Gadolinium complex of ¹²⁵I/¹²⁷I-RGD-DOTA conjugate as a tumor-targeting SPECT/MR bimodal imaging probe

Ji Ae Park, Jung Young Kim, Yong Jin Lee, Wonho Lee, Sang Moo Lim, Tae Jeong Kim, Jeongsoo Yoo, Yongmin Chang, Kyeong Min Kim

School of Health and Environmental Science

Research output: Contribution to journal › Article

22 Citations (Scopus)

Abstract

The work describes the synthesis and in vivo application of [Gd(L)(H ₂O)]·xH₂O, where L is a (¹²⁵I/ ¹²⁷I-RGD)- DOTA conjugate, as a tumor-targeting SPECT/MR bimodal imaging probe. Here, (¹²⁵I/¹²⁷I-RGD)-DOTA signifies a "cocktail mixture" of radioisotopic (1a, L = ¹²⁵I-RGD-DOTA) and natural (1b, L = ¹²⁷I-RGD-DOTA) Gd complexes. The two complexes are chemically equivalent as revealed by HPLC, and their cocktail mixture exhibits the integrin-specific tumor enhancement, demonstrating that they constitute essentially a single bimodal imaging probe. Employment of a cocktail mixture thus proves to be a sole and practical approach to overcome the sensitivity difference problem between MRI and SPECT.

Original language	English
Pages (from-to)	216-219
Number of pages	4
Journal	ACS Medicinal Chemistry Letters
Volume	4
Issue number	2
DOIs	https://doi.org/10.1021/ml3003499
Publication status	Published - 2013 Feb 14

Keywords

RGD peptide
SPECT/MR
dual modality
small molecule
tumor targeting

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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10.1021/ml3003499

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Park, J. A., Kim, J. Y., Lee, Y. J., Lee, W., Lim, S. M., Kim, T. J., Yoo, J., Chang, Y., & Kim, K. M. (2013). Gadolinium complex of ¹²⁵I/¹²⁷I-RGD-DOTA conjugate as a tumor-targeting SPECT/MR bimodal imaging probe. ACS Medicinal Chemistry Letters, 4(2), 216-219. https://doi.org/10.1021/ml3003499

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abstract = "The work describes the synthesis and in vivo application of [Gd(L)(H 2O)]·xH2O, where L is a (125I/ 127I-RGD)- DOTA conjugate, as a tumor-targeting SPECT/MR bimodal imaging probe. Here, (125I/127I-RGD)-DOTA signifies a {"}cocktail mixture{"} of radioisotopic (1a, L = 125I-RGD-DOTA) and natural (1b, L = 127I-RGD-DOTA) Gd complexes. The two complexes are chemically equivalent as revealed by HPLC, and their cocktail mixture exhibits the integrin-specific tumor enhancement, demonstrating that they constitute essentially a single bimodal imaging probe. Employment of a cocktail mixture thus proves to be a sole and practical approach to overcome the sensitivity difference problem between MRI and SPECT.",

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AU - Lee, Wonho

AU - Lim, Sang Moo

AU - Kim, Tae Jeong

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AB - The work describes the synthesis and in vivo application of [Gd(L)(H 2O)]·xH2O, where L is a (125I/ 127I-RGD)- DOTA conjugate, as a tumor-targeting SPECT/MR bimodal imaging probe. Here, (125I/127I-RGD)-DOTA signifies a "cocktail mixture" of radioisotopic (1a, L = 125I-RGD-DOTA) and natural (1b, L = 127I-RGD-DOTA) Gd complexes. The two complexes are chemically equivalent as revealed by HPLC, and their cocktail mixture exhibits the integrin-specific tumor enhancement, demonstrating that they constitute essentially a single bimodal imaging probe. Employment of a cocktail mixture thus proves to be a sole and practical approach to overcome the sensitivity difference problem between MRI and SPECT.

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