DNA
DNA测序
计算生物学
配体(生物化学)
组合化学
化学
靶蛋白
酶
生物化学
生物
分子生物学
基因
受体
作者
Luca Prati,Martina Bigatti,Etienne J. Donckèle,Dario Neri,Florent Samain
标识
DOI:10.1016/j.bbrc.2020.04.030
摘要
DNA-encoded chemical libraries (DECLs) are large compound collections attached to DNA fragments, serving as amplifiable barcodes, which can be screened on target proteins of pharmaceutical interest. In DECL selections, ligands are identified by high-throughput DNA sequencing, by comparing their frequency before and after the affinity capture step. Hits identified using this procedure need to be validated by resynthesis and by performing affinity measurements. Here we report novel on-DNA hit validation strategies, which enable the facile confirmation of ligand-protein interaction as well as the determination of equilibrium and kinetic binding constants. The experimental procedures, which had been inspired by enzyme-linked immunosorbent assays (ELISA), were validated using ligands of different affinity to carbonic anhydrase II and IX.
科研通智能强力驱动
Strongly Powered by AbleSci AI