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使用β-淀粉样蛋白成像探针进行胰岛中胰淀素成像的可行性。

Feasibility of amylin imaging in pancreatic islets with β-amyloid imaging probes.

作者信息

Yoshimura Masashi, Ono Masahiro, Watanabe Hiroyuki, Kimura Hiroyuki, Saji Hideo

机构信息

Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.

出版信息

Sci Rep. 2014 Aug 21;4:6155. doi: 10.1038/srep06155.

DOI:10.1038/srep06155
PMID:25142178
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4139942/
Abstract

Islet amyloid deposition composed of amylin aggregates is regarded as one of the hallmarks of type 2 diabetes mellitus (T2DM). For the diagnosis of T2DM, several nuclear medical imaging probes have been developed. However, there have been no reports regarding the development of imaging probes targeting amylin. In this report, we investigated the feasibility of amylin imaging using [(125)I]IPBF as one of the model compounds of β-amyloid (Aβ) imaging probes. In in vitro experiments, [(125)I]IPBF exhibited high binding affinity for amylin aggregates (Kd = 8.31 nM). Moreover, autoradiographic images showed that [(125)I]IPBF specifically bound to islet amyloid composed of amylin. These results suggest the potential application of Aβ imaging probes to amylin imaging. In addition, [(125)I]IPBF is one of the promising lead compounds for amylin imaging, and further structural optimization based on [(125)I]IPBF may lead to useful tracers for the in vivo imaging of islet amyloids in the pancreas.

摘要

由胰岛淀粉样多肽聚集体构成的胰岛淀粉样沉积被视为2型糖尿病（T2DM）的标志之一。为了诊断T2DM，已经开发了几种核医学成像探针。然而，关于靶向胰岛淀粉样多肽的成像探针的开发尚无报道。在本报告中，我们研究了使用[(125)I]IPBF作为β-淀粉样蛋白（Aβ）成像探针的模型化合物之一进行胰岛淀粉样多肽成像的可行性。在体外实验中，[(125)I]IPBF对胰岛淀粉样多肽聚集体表现出高结合亲和力（解离常数Kd = 8.31 nM）。此外，放射自显影图像显示[(125)I]IPBF特异性结合由胰岛淀粉样多肽构成的胰岛淀粉样物质。这些结果表明Aβ成像探针在胰岛淀粉样多肽成像方面的潜在应用。此外，[(125)I]IPBF是用于胰岛淀粉样多肽成像的有前景的先导化合物之一，基于[(125)I]IPBF进行进一步的结构优化可能会产生用于胰腺中胰岛淀粉样物质体内成像的有用示踪剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/a885c4438ed6/srep06155-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/ab9d21aaa984/srep06155-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/a374653d1d3e/srep06155-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/745c2aebc9ce/srep06155-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/3945d60fb1db/srep06155-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/a885c4438ed6/srep06155-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/ab9d21aaa984/srep06155-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/a374653d1d3e/srep06155-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/745c2aebc9ce/srep06155-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/3945d60fb1db/srep06155-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0f2/4139942/a885c4438ed6/srep06155-f5.jpg

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