PDF(Pubmed)
Abstract：
We describe a versatile and tuneable thiol responsive linker system using thiovinylketones, which relies on the conjugate addition-elimination mechanism of Michael acceptors for the traceless release of therapeutics. In a proof-of-principle study, we translate our findings to exhibit potent thiol-cleavable antibiotic prodrugs and antibody-drug conjugates.
摘要：
我们描述了一种使用硫代乙烯基酮的通用和可调的硫醇响应接头系统，这依赖于迈克尔受体的共轭加成-消除机制，用于无痕释放治疗剂。在一项原理证明研究中，我们将我们的发现转化为展示有效的巯基可裂解的抗生素前药和抗体-药物偶联物.
