Improved tumor-targeting MRI contrast agents: Gd(DOTA) conjugates of a cycloalkane-based RGD peptide

Ji Ae Park; Yong Jin Lee; In Ok Ko; Tae Jeong Kim; Yongmin Chang; Sang Moo Lim; Kyeong Min Kim; Jung Young Kim

doi:10.1016/j.bbrc.2014.10.155

Improved tumor-targeting MRI contrast agents: Gd(DOTA) conjugates of a cycloalkane-based RGD peptide

Ji Ae Park, Yong Jin Lee, In Ok Ko, Tae Jeong Kim, Yongmin Chang, Sang Moo Lim, Kyeong Min Kim, Jung Young Kim

Department of Medicine

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

19 Scopus citations

Abstract

Two new MRI contrast agents, Gd-DOTA-c(RGD-ACP-K) (1) and Gd-DOTA-c(RGD-ACH-K) (2), which were designed by incorporating aminocyclopentane (ACP)- or aminocyclohexane (ACH)-carboxylic acid into Gd-DOTA (gadolinium-tetraazacyclo dodecanetetraacetic acid) and cyclic RGDK peptides, were synthesized and evaluated for tumor-targeting ability in vitro and in vivo. Binding affinity studies showed that both 1 and 2 exhibited higher affinity for integrin receptors than cyclic RGDyK peptides, which were used as a reference. These complexes showed high relaxivity and good stability in human serum and have the potential to improve target-specific signal enhancement in vivo MR images.

Original language	English
Pages (from-to)	246-250
Number of pages	5
Journal	Biochemical and Biophysical Research Communications
Volume	455
Issue number	3-4
DOIs	https://doi.org/10.1016/j.bbrc.2014.10.155
State	Published - 12 Dec 2014

Keywords

Contrast agents
Cyclic
Gd-DOTA
MRI
RGD peptide
Tumor targeting

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10.1016/j.bbrc.2014.10.155

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title = "Improved tumor-targeting MRI contrast agents: Gd(DOTA) conjugates of a cycloalkane-based RGD peptide",

abstract = "Two new MRI contrast agents, Gd-DOTA-c(RGD-ACP-K) (1) and Gd-DOTA-c(RGD-ACH-K) (2), which were designed by incorporating aminocyclopentane (ACP)- or aminocyclohexane (ACH)-carboxylic acid into Gd-DOTA (gadolinium-tetraazacyclo dodecanetetraacetic acid) and cyclic RGDK peptides, were synthesized and evaluated for tumor-targeting ability in vitro and in vivo. Binding affinity studies showed that both 1 and 2 exhibited higher affinity for integrin receptors than cyclic RGDyK peptides, which were used as a reference. These complexes showed high relaxivity and good stability in human serum and have the potential to improve target-specific signal enhancement in vivo MR images.",

keywords = "Contrast agents, Cyclic, Gd-DOTA, MRI, RGD peptide, Tumor targeting",

author = "Park, {Ji Ae} and Lee, {Yong Jin} and Ko, {In Ok} and Kim, {Tae Jeong} and Yongmin Chang and Lim, {Sang Moo} and Kim, {Kyeong Min} and Kim, {Jung Young}",

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doi = "10.1016/j.bbrc.2014.10.155",

language = "English",

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T2 - Gd(DOTA) conjugates of a cycloalkane-based RGD peptide

AU - Park, Ji Ae

AU - Lee, Yong Jin

AU - Ko, In Ok

AU - Kim, Tae Jeong

AU - Chang, Yongmin

AU - Lim, Sang Moo

AU - Kim, Kyeong Min

AU - Kim, Jung Young

PY - 2014/12/12

Y1 - 2014/12/12

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AB - Two new MRI contrast agents, Gd-DOTA-c(RGD-ACP-K) (1) and Gd-DOTA-c(RGD-ACH-K) (2), which were designed by incorporating aminocyclopentane (ACP)- or aminocyclohexane (ACH)-carboxylic acid into Gd-DOTA (gadolinium-tetraazacyclo dodecanetetraacetic acid) and cyclic RGDK peptides, were synthesized and evaluated for tumor-targeting ability in vitro and in vivo. Binding affinity studies showed that both 1 and 2 exhibited higher affinity for integrin receptors than cyclic RGDyK peptides, which were used as a reference. These complexes showed high relaxivity and good stability in human serum and have the potential to improve target-specific signal enhancement in vivo MR images.

KW - Contrast agents

KW - Cyclic

KW - Gd-DOTA

KW - MRI

KW - RGD peptide

KW - Tumor targeting

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JF - Biochemical and Biophysical Research Communications

IS - 3-4

ER -

Improved tumor-targeting MRI contrast agents: Gd(DOTA) conjugates of a cycloalkane-based RGD peptide

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Keywords

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