A Concise Synthesis of Site-Specific and Topologically-Defined Protein-Poly(amino acid) Conjugates

Peng R. Chen

doi:10.11777/j.issn1000-3304.2016.16272

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A Concise Synthesis of Site-Specific and Topologically-Defined Protein-Poly(amino acid) Conjugates

Research Highlights | 更新时间：2021-03-19

- A Concise Synthesis of Site-Specific and Topologically-Defined Protein-Poly(amino acid) Conjugates
- Acta Polymerica Sinica Issue 11, Pages: 1465-1467(2016)
- 作者机构：
  
  北京大学化学与分子工程学院北京 100871
- 作者简介：
- 基金信息：
- DOI：10.11777/j.issn1000-3304.2016.16272
  CLC：
- Published：2016-11，
  
  Received：5 September 2016，
  
  Revised：17 September 2016，
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Peng R. Chen. A Concise Synthesis of Site-Specific and Topologically-Defined Protein-Poly(amino acid) Conjugates. [J]. Acta Polymerica Sinica (11):1465-1467(2016)
DOI：

Peng R. Chen. A Concise Synthesis of Site-Specific and Topologically-Defined Protein-Poly(amino acid) Conjugates. [J]. Acta Polymerica Sinica (11):1465-1467(2016) DOI： 10.11777/j.issn1000-3304.2016.16272.

摘要

发展位点特异且具有明确拓扑结构的蛋白质-高分子偶联物是高分子和化学生物学领域共同面对的挑战之一.在聚合物末端精确引入一个或多个具有特殊反应活性的生物正交官能团是实现“位点特异”生物偶联的关键前提.这一过程通常比较低效、需要多步骤的官能团转化、聚合后修饰以及保护脱保护，费时且繁琐.最近，通过在聚合过程中原位生成官能团，以一锅-两步的过程得到可直接用于蛋白质偶联的异遥爪聚合物，从而实现了多种不同拓扑结构的蛋白质-聚氨基酸偶联物的快速构筑.这一简洁的合成路线实现了以前尚未获得的头-尾相接的环状偶联物的制备，使这些偶联物表现出了很强的体外酶稳定性以及热稳定性.该工作是蛋白质-高分子偶联化学的一次创新的尝试；同时，利用该方法所制备的偶联物在蛋白质药物领域具有广阔的应用前景.

Abstract

The development of site-specific and topologically-defined protein-polymer conjugates has been challenging

which is mainly due to the tedious and low-efficient synthesis. Typically

multi-step modifications on the polymer part are necessary in order to install functionalities required for subsequent bioconjugation. A recent work has addressed this challenge by producing well-defined heterotelechelic poly(amino acid)s

via

a one-pot

two-step polymerization process that allows

in situ

installation of two different bioorthogonal functionalities. Various site-specific and topologically-defined protein-poly(amino acid) conjugates exhibiting remarkably improved protease resistance and thermostability were generated with substantially reduced synthetic efforts. The method may provide a general platform and a concise strategy to prepare protein-polymer conjugates with bright therapeutic potentials.

关键词

简洁合成蛋白质-高分子偶联物聚氨基酸原位官能团生成

Keywords

Concise synthesisProtein-polymer conjugatesPoly(amino acid)In situ-functionalization

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Related Institution

School and Hospital of Stomatology, Peking University

Department of Biomedical Engineering, Peking University

Department of Polymeric Materials, School of Materials Science and Engineering, Tongji University

Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences

School of Applied Chemistry and Engineering, University of Science and Technology of China

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