Synthesis of protectin D1 analogs: novel pro-resolution and radiotracer agents.

Synthesis of protectin D1 analogs: novel pro-resolution and radiotracer agents.
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保护素 D1 类似物的合成:新型促解析剂和放射性示踪剂。

DOI:
10.1039/c8ob01232f
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发表时间:
2018
影响因子:
3.2
通讯作者:
Hansen,TV
Hansen,TV
中科院分区:
化学3区
文献类型:
--
作者:
Tungen,JE;Aursnes,M;Ramon,S;Colas,RA;Serhan,CN;Olberg,DE;Nuruddin,S;Willoch,F;Hansen,TV

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保护蛋白D1是一种特殊的促溶解介质,在几种人类疾病模型中具有有效的促溶解和抗炎作用。本文介绍了首个合成保护蛋白D1类似物的制备,命名为22-F-PD1,并介绍了体内研究的数据。这种类似物显示出有效的促溶解和抗炎特性。这些结果启发了放射性示踪剂22-[18F]F-PD1-ME的制备,该示踪剂用于正电子发射断层扫描概念验证研究。总之,这些发现有助于对保护蛋白D1类似物的生物分子特性有新的认识。此外,一种改进的代谢物22-OH-PD1的正式合成被报道。
Protectin D1 is a specialized pro-resolving mediator with potent pro-resolving and anti-inflammatory effects in vivo in several human disease models. Herein the preparation of the first synthetic analog of protectin D1, named 22-F-PD1, is presented together with data from in vivo investigations. This analog showed potent pro-resolving and anti-inflammatory properties. These results inspired the preparation of the radiotracer 22-[18F]F-PD1-ME that was used in a positron emission tomography proof of concept study. Altogether, the findings presented contribute to new knowledge on the biomolecular properties of protectin D1 analogs. In addition, an improved formal synthesis of the metabolite 22-OH-PD1 is reported.
DOI: 10.1021/cr100396c
发表时间: 2011-10-12
期刊: CHEMICAL REVIEWS
影响因子: 62.1
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