Merck Research Laboratories, Kenilworth, NJ, USA.
Methods Mol Biol. 2022;2541:165-172. doi: 10.1007/978-1-0716-2545-3_20.
Compounds acting through irreversible covalent interactions with therapeutic targets represent an important mechanism of drug action. Here I describe a selection method for DNA-encoded libraries to discover irreversible covalent binders to target proteins. This method offers an enabling tool in drug discovery for therapeutic targets that may be undruggable for reversible inhibition.
通过与治疗靶点发生不可逆共价相互作用而发挥作用的化合物代表了药物作用的一个重要机制。在这里，我描述了一种用于发现与靶蛋白发生不可逆共价结合的 DNA 编码文库的筛选方法。该方法为可能难以通过可逆抑制来治疗的治疗靶点的药物发现提供了一种可行的工具。
