Digging into the Sequential Space of Thiolactone Precision Polymers: A Combinatorial Strategy to Identify Functional Domains
Digging into the Sequential Space of Thiolactone Precision Polymers: A Combinatorial Strategy to Identify Functional Domains
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DOI：
10.1002/anie.201810393
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发表时间：
2019-02-11
影响因子：
16.6
通讯作者：
Boerner, Hans G.
中科院分区：
文献类型：
--
作者：
Celasun, Sensu;Remmler, Dario;Boerner, Hans G.
基于硫内酯/迈克尔化学的精密聚合物的功能序列从一个大的单珠单化合物库中鉴定。通过MALDI-TOF MS/MS的单珠读出鉴定了作为第二代光敏剂药物的宿主m-THPC的序列。相应的Tla/Michael-PEG缀合物使m-THPC在溶液中可用，并且药物有效载荷以及药物释放动力学可以通过精密部分进行微调。
Functional sequences of precision polymers based on thiolactone/Michael chemistry are identified from a large one-bead one-compound library. Single-bead readout by MALDI-TOF MS/MS identifies sequences that host m-THPC that is a second generation photo-sensitizer drug. The corresponding Tla/Michael-PEG conjugates make m-THPC available in solution and drug payload as well as drug release kinetics can be fine-tuned by the precision segment.