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

Korea Institute of Radiological and Medical Sciences
Kyungpook National University

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

22 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\}",

note = "Publisher Copyright: {\textcopyright} 2014 Elsevier Inc.",

year = "2014",

month = dec,

day = "12",

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

language = "English",

volume = "455",

pages = "246--250",

journal = "Biochemical and Biophysical Research Communications",

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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

UR - https://www.scopus.com/pages/publications/84914148016

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DO - 10.1016/j.bbrc.2014.10.155

M3 - Article

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AN - SCOPUS:84914148016

SN - 0006-291X

VL - 455

SP - 246

EP - 250

JO - Biochemical and Biophysical Research Communications

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

Abstract

Keywords

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