preparing-68ga-labeled-arginine-glycine-aspartate-rgd-peptide-for

Preparing a <sup>68</sup>Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis

The &#945;v&#946;3 integrin is a heterodimeric adhesion molecule involved in tumor cell migration and angiogenesis. The integrin is overexpressed in ...

Korea Institute of Radiological and Medical Sciences

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. 

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

Although amyloid beta (Aβ) imaging is widely used for diagnosing and monitoring Alzheimer's disease in clinical fields, paralleling comparison between F-flutemetamol and F-florbetaben was rarely attempted in AD mouse model. We performed a comparison of Aβ PET images between F-flutemetamol and F-florbetaben in a recently developed APPswe mouse model, C57BL/6-Tg (NSE-hAPPsw) Korl.

Assessment of brain beta-amyloid deposition in transgenic mouse models of Alzheimer's disease with PET imaging agents F-flutemetamol and F-florbetaben.

In this study, we designed and synthesized a highly stable manganese (Mn)-based hepatobiliary complex by tethering an ethoxybenzyl (EOB) moiety with an ethylenediaminetetraacetic acid (EDTA) coordination cage as an alternative to the well-established hepatobiliary gadolinium (Gd) chelates and evaluated its usage as a T hepatobiliary magnetic resonance imaging (MRI) contrast agent (CA). This new complex exhibits higher r relaxivity (2.3 mM s) than clinically approved Mn-based hepatobiliary complex Mn-DPDP (1.6 mM s) at 1.5 T. Mn-EDTA-EOB shows much higher kinetic inertness than that of clinically approved Gd-based hepatobiliary MRI CAs, such as Gd-DTPA-EOB and Gd-BOPTA. In addition, in vivo biodistribution and MRI enhancement patterns of this new Mn chelate are comparable to those of Gd-based hepatobiliary MRI CAs. The diagnostic efficacy of the new complex was demonstrated by its enhanced tumor detection sensitivity in a liver cancer model using in vivo MRI.

Synthesis and Evaluation of Manganese(II)-Based Ethylenediaminetetraacetic Acid-Ethoxybenzyl Conjugate as a Highly Stable Hepatobiliary Magnetic Resonance Imaging Contrast Agent.

Ji-Ae Park

Division of Applied RI

Korea Institute of Radiological and Medical Sciences

Preparing a ⁶⁸Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis

Ji-Ae Park

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Korea Institute of Radiological and Medical Sciences

Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis

Division of Applied RI

Preparing a ⁶⁸Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis