MOE Key Laboratory of Protein Sciences, School of Life Sciences, Tsinghua University, Beijing 100084, P. R. China.
Chem Commun (Camb). 2019 Dec 5;55(98):14848-14851. doi: 10.1039/c9cc08509b.
HDAC6 (histone deacetylase 6) catalyses the deacetylation of non-histone substrates, and plays important roles in cell migration, protein degradation and other cellular processes. Here we report that CRBN-recruiting PROTAC NH2, which introduces pomalidomide at the benzene ring of Nex A, reaches comparable degradation efficiency of HDAC6 compared to aliphatic-chain-introducing PROTAC NP8.
HDAC6（组蛋白去乙酰化酶 6）催化非组蛋白底物的去乙酰化，在细胞迁移、蛋白质降解和其他细胞过程中发挥重要作用。在这里，我们报告说，CRBN 募集的 PROTAC NH2 在 Nex A 的苯环上引入了泊马度胺，与引入脂肪链的 PROTAC NP8 相比，对 HDAC6 的降解效率相当。
