Ternary Complex‐Templated Dynamic Combinatorial Chemistry for the Selection and Identification of Homo‐PROTACs
作者:Claudia J. Diehl、Alessandra Salerno、Alessio Ciulli
DOI:10.1002/anie.202319456
日期:——
Dynamic Combinatorial Chemistry meets PROTAC screening: Stability of ternary complexes formed by PROTACs is shown to act as selection criterion in multi-protein templated dynamic combinatorial libraries. Reversible thiol-disulfide exchange chemistry allows rapid identification of novel VHL-targeting Homo-PROTACs from complex library mixtures.
动态组合化学符合 PROTAC 筛选:PROTAC 形成的三元复合物的稳定性被证明可作为多蛋白模板动态组合库中的选择标准。可逆的硫醇-二硫化物交换化学允许从复杂的文库混合物中快速鉴定新型 VHL 靶向 Homo-PROTAC。