Park Ji-Ae, Lee Yong Jin, Ko In Ok, Kim Tae-Jeong, Chang Yongmin, Lim Sang Moo, Kim Kyeong Min, Kim Jung Young
Molecular Imaging Research Center, Korea Institute of Radiological & Medical Sciences, Seoul, Republic of Korea.
Molecular Imaging Research Center, Korea Institute of Radiological & Medical Sciences, Seoul, Republic of Korea.
Biochem Biophys Res Commun. 2014 Dec 12;455(3-4):246-50. doi: 10.1016/j.bbrc.2014.10.155. Epub 2014 Nov 6.
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.
两种新型磁共振成像（MRI）造影剂，即通过将氨基环戊烷（ACP）或氨基环己烷（ACH）羧酸引入钆-四氮杂环十二烷四乙酸（Gd-DOTA）和环状RGDK肽而设计的Gd-DOTA-c(RGD-ACP-K)（1）和Gd-DOTA-c(RGD-ACH-K)（2），已被合成，并在体外和体内对其肿瘤靶向能力进行了评估。结合亲和力研究表明，与用作参考的环状RGDyK肽相比，1和2对整合素受体均表现出更高的亲和力。这些复合物在人血清中显示出高弛豫率和良好的稳定性，并且有潜力改善体内磁共振图像中的靶向特异性信号增强。
