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The potent small molecule integrin antagonist THR-687 is a promising next-generation therapy for retinal vascular disorders.强效小分子整合素拮抗剂 THR-687 是一种很有前途的新一代治疗视网膜血管疾病的药物。
Exp Eye Res. 2019 Mar;180:43-52. doi: 10.1016/j.exer.2018.11.022. Epub 2018 Nov 22.
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The effects of bevacizumab treatment in a rat model of retinal ischemia and perfusion injury.贝伐单抗治疗对视网膜缺血灌注损伤大鼠模型的影响。
Mol Vis. 2018 Mar 23;24:239-250. eCollection 2018.
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Preparation and evaluation of a Ga-labeled RGD-containing octapeptide for noninvasive imaging of angiogenesis: biodistribution in non-human primate.用于血管生成无创成像的镓标记含RGD八肽的制备与评价：在非人类灵长类动物中的生物分布
Am J Nucl Med Mol Imaging. 2018 Feb 5;8(1):15-31. eCollection 2018.
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Protective Effect of Prunus Cerasus (Sour Cherry) Seed Extract on the Recovery of Ischemia/Reperfusion-Induced Retinal Damage in Zucker Diabetic Fatty Rat.樱桃李籽油对 Zucker 糖尿病肥胖大鼠缺血再灌注诱导的视网膜损伤恢复的保护作用。
Molecules. 2017 Oct 21;22(10):1782. doi: 10.3390/molecules22101782.
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Dynamics of angiogenesis in ischemic areas of the infarcted heart.梗死心脏缺血区血管生成的动力学。
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Imaging of αβ integrin expression in experimental myocardial ischemia with [Ga]NODAGA-RGD positron emission tomography.利用[镓]NODAGA-RGD正电子发射断层扫描对实验性心肌缺血中αβ整合素表达进行成像。
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A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins.RGD 结合整合素配体的活性和选择性特征的综合评价。
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Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice.贝司他汀对链脲佐菌素诱导的糖尿病小鼠视网膜的保护作用。
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使用 Ga-NOTA-c(NGR) 对手术大鼠模型中缺血/再灌注介导的氨肽酶 N 表达进行成像。

Imaging of Ischemia/Reperfusion-mediated Aminopeptidase N Expression in Surgical Rat Model Using Ga-NOTA-c(NGR).

机构信息

Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Debrecen, Hungary.

Gyula Petrányi Doctoral School of Allergy and Clinical Immunology, Faculty of Medicine, University of Debrecen, Debrecen, Hungary.

出版信息

In Vivo. 2022 Mar-Apr;36(2):657-666. doi: 10.21873/invivo.12750.

DOI:10.21873/invivo.12750
PMID:35241519
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8931911/
Abstract

BACKGROUND/AIM: Previous studies have already shown that Gallium(Ga)-labeled NGR-based radiopharmaceuticals specifically bind to the neoangiogenic molecule Aminopeptidase N (APN/CD13). The aim of this study was to evaluate the applicability of Ga-NOTA-c(NGR) in the in vivo detection of the temporal changes of APN/CD13 expression in the diabetic retinopathy rat model using positron emission tomography (PET).

MATERIALS AND METHODS

Ischemia/reperfusion injury was initiated by surgical ligation of the left bulbus oculi of rats. In vivo PET imaging studies were performed after the surgery using Ga-NOTA-c(NGR).

RESULTS

Significantly higher Ga-NOTA-c(NGR) uptake was observed in the surgically-ligated left bulbus, compared to the bulbus of the non-surgical group at each investigated time point. The western blot and histological analysis confirmed the increased expression of the neo-angiogenic marker APN/CD13.

CONCLUSION

Ga-NOTA-c(NGR) is a suitable radiotracer for the detection of the temporal changes of the ischemia/reperfusion-mediated expression of APN/CD13 in the surgically induced diabetic retinopathy rat model.

摘要

背景/目的：之前的研究已经表明，镓（Ga）标记的基于 NGR 的放射性药物特异性结合新生血管生成分子氨基肽酶 N（APN/CD13）。本研究旨在评估 Ga-NOTA-c（NGR）在使用正电子发射断层扫描（PET）检测糖尿病视网膜病变大鼠模型中 APN/CD13 表达的时间变化中的适用性。

材料和方法

通过手术结扎大鼠左眼球来引发缺血/再灌注损伤。手术后使用 Ga-NOTA-c（NGR）进行体内 PET 成像研究。

结果

与非手术组相比，在每个研究时间点，手术结扎的左眼球中观察到 Ga-NOTA-c（NGR）的摄取明显更高。Western blot 和组织学分析证实了新生血管标志物 APN/CD13 的表达增加。

结论

Ga-NOTA-c（NGR）是一种合适的示踪剂，可用于检测手术诱导的糖尿病视网膜病变大鼠模型中缺血/再灌注介导的 APN/CD13 表达的时间变化。