Department of Material and Life Chemistry, Faculty of Engineering, Kanagawa University, 3-27-1 Rokkakubashi, Kanagawa-ku, Yokohama 221-8686, Japan.
Org Lett. 2020 Aug 7;22(15):6006-6009. doi: 10.1021/acs.orglett.0c02086. Epub 2020 Jul 14.
Protection and deprotection of the 2'-hydroxyl group of RNAs are critical for RNA-based drug discovery. This paper reports development of a bioreduction labile protecting group of the 2'-hydroxyl group in RNA. After the reduction of the nitro group in a chemical or enzymatic manner, the protecting groups were removed spontaneously. The attachment of electron-donating groups to the benzene ring or benzylic carbon enabled fast and controllable deprotection of the 2'-hydroxyl protecting group under physiological conditions.
保护和去保护 RNA 的 2'-羟基对于基于 RNA 的药物发现至关重要。本文报道了一种生物还原不稳定的 RNA 2'-羟基保护基的开发。在通过化学或酶促方式还原硝基后，保护基会自动去除。在苯环或苄基碳上引入供电子基团可以在生理条件下快速且可控地脱去 2'-羟基保护基。
