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通用接头多样化方法用于双价配体组装:阳离子非依赖性甘露糖 6-磷酸受体配体阵列的生成。

General Linker Diversification Approach to Bivalent Ligand Assembly: Generation of an Array of Ligands for the Cation-Independent Mannose 6-Phosphate Receptor.

机构信息

Department of Chemistry, University of Nebraska , Lincoln, Nebraska 68588-0304, United States.

Department of Biochemistry & Molecular Biology, University of Nebraska Medical Center , Omaha, Nebraska 68198-5870, United States.

出版信息

Org Lett. 2017 Aug 18;19(16):4267-4270. doi: 10.1021/acs.orglett.7b01914. Epub 2017 Jul 28.

Abstract

A generalized strategy is presented for the rapid assembly of a set of bivalent ligands with a variety of linking functionalities from a common monomer. Herein, an array of phosphatase-inert mannose-6-phosphonate-presenting ligands for the cation-independent-mannose 6-phosphate receptor (CI-MPR) is constructed. Receptor binding affinity varies with linking functionality-the simple amide and 1,5-triazole(tetrazole) being preferred over the 1,4-triazole. This approach is expected to find application across chemical biology, particularly in glycoscience, wherein multivalency often governs molecular recognition.

摘要

本文提出了一种通用策略,用于从常见单体快速组装具有多种连接功能的一组二价配体。本文构建了一系列用于阳离子非依赖性甘露糖 6-磷酸受体(CI-MPR)的磷酸酶惰性甘露糖-6-磷酸展示配体。受体结合亲和力随连接功能的不同而变化——酰胺和 1,5-三唑(四唑)比 1,4-三唑更受欢迎。这种方法有望在化学生物学中得到应用,特别是在糖科学中,其中多价性通常控制分子识别。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48f0/6208139/e2e2d59e7527/nihms-990847-f0008.jpg

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本文引用的文献

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