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信号肽glorin的通用合成

Versatile synthesis of the signaling peptide glorin.

作者信息

Barnett Robert, Raszkowski Daniel, Winckler Thomas, Stallforth Pierre

机构信息

Leibniz Institute for Natural Product Research and Infection Biology, Hans Knöll Institute - HKI, Junior Research Group Chemistry of Microbial Communication, Beutenbergstr. 11, D-07745 Jena, Germany.

Faculty of Biology and Pharmacy, Institute of Pharmacy, Department of Pharmaceutical Biology, University of Jena, Semmelweisstrasse 10, D-07743 Jena, Germany.

出版信息

Beilstein J Org Chem. 2017 Feb 8;13:247-250. doi: 10.3762/bjoc.13.27. eCollection 2017.

DOI:10.3762/bjoc.13.27
PMID:28326133
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5331329/
Abstract

We present a versatile synthesis of the eukaryotic signaling peptide glorin as well as glorinamide, a synthetic analog. The ability of these compounds to activate glorin-induced genes in the social amoeba was evaluated by quantitative reverse transcription PCR, whereby both compounds showed bioactivity comparable to a glorin standard. This synthetic route will be useful in conducting detailed structure-activity relationship studies as well as in the design of chemical probes to dissect glorin-mediated signaling pathways.

摘要

我们展示了真核信号肽荣耀素（glorin）以及其合成类似物荣耀素酰胺（glorinamide）的通用合成方法。通过定量逆转录聚合酶链反应评估了这些化合物激活群居变形虫中荣耀素诱导基因的能力，结果表明这两种化合物均表现出与荣耀素标准品相当的生物活性。这种合成途径将有助于进行详细的构效关系研究以及设计化学探针来剖析荣耀素介导的信号通路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/2281a1b8a5e8/Beilstein_J_Org_Chem-13-247-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/2243dfee5241/Beilstein_J_Org_Chem-13-247-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/06c6a9f1297f/Beilstein_J_Org_Chem-13-247-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/2281a1b8a5e8/Beilstein_J_Org_Chem-13-247-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/2243dfee5241/Beilstein_J_Org_Chem-13-247-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/06c6a9f1297f/Beilstein_J_Org_Chem-13-247-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8142/5331329/2281a1b8a5e8/Beilstein_J_Org_Chem-13-247-g003.jpg

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本文引用的文献

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Bacterial Alkaloids Prevent Amoebal Predation.细菌生物碱可防止食藻原生动物的捕食。
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Antinematode activity of Violacein and the role of the insulin/IGF-1 pathway in controlling violacein sensitivity in Caenorhabditis elegans.紫菌素的抗线虫活性以及胰岛素/胰岛素样生长因子-1信号通路在秀丽隐杆线虫中控制紫菌素敏感性的作用。
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Protist. 2012 Jan;163(1):25-37. doi: 10.1016/j.protis.2010.12.002. Epub 2011 Mar 2.
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Protozoan-induced regulation of cyclic lipopeptide biosynthesis is an effective predation defense mechanism for Pseudomonas fluorescens.原核生物诱导环脂肽生物合成的调节是荧光假单胞菌有效捕食防御机制。
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