AN UNNATURAL BIOPOLYMER
AN UNNATURAL BIOPOLYMER
复制标题
DOI：
10.1126/science.7689747
复制
发表时间：
1993-09-03
期刊：
影响因子：
56.9
通讯作者：
SCHULTZ, PG
中科院分区：
文献类型：
--
作者：
CHO, CY;MORAN, EJ;SCHULTZ, PG
一种高效的方法已经开发出来，用于固相合成“非天然生物聚合物”，该聚合物由通过氨基甲酸酯主链连接的手性氨基碳酸酯单体组成。低聚氨基甲酸酯由 N 保护的碳酸对硝基苯酯单体合成，并用多种侧链取代，每步总偶联效率超过 99%。使用光化学方法生成空间限定的低聚氨基甲酸酯文库，并筛选与单克隆抗体的结合亲和力。然后合成了许多高亲和力配体，并在溶液中分析了它们的抑制浓度值、水/辛醇分配系数和蛋白水解稳定性。这些和其他非天然聚合物可以为药物开发以及测试蛋白质和肽折叠和结构的理论提供新的框架。
A highly efficient method has been developed for the solid-phase synthesis of an ''unnatural biopolymer'' consisting of chiral aminocarbonate monomers linked via a carbamate backbone. Oligocarbamates were synthesized from N-protected p-nitrophenyl carbonate monomers, substituted with a variety of side chains, with greater than 99 percent overall coupling efficiencies per step. A spatially defined library of oligocarbamates was generated by using photochemical methods and screened for binding affinity to a monoclonal antibody. A number of high-affinity ligands were then synthesized and analyzed in solution with respect to their inhibition concentration values, water/octanol partitioning coefficients, and proteolytic stability. These and other unnatural polymers may provide new frameworks for drug development and for testing theories of protein and peptide folding and structure.