cereblon 招募的蛋白水解靶向嵌合体（PROTACs）可特异性地使 HDAC1 降解，而不降解 HDAC3。
Cereblon-recruiting proteolysis targeting chimeras (PROTACs) can determine the selective degradation of HDAC1 over HDAC3.
机构信息
Leicester Institute of Structural and Chemical Biology and School of Chemistry, University of Leicester, University Road, Leicester, LE1 7RH, UK.
São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, Brazil.
出版信息
Chem Commun (Camb). 2024 Nov 21;60(94):13879-13882. doi: 10.1039/d4cc05138f.
Histone deacetylase (HDAC) enzymes 1-3 exist in several corepressor complexes and are viable drug targets. To date, proteolysis targeting chimeras (PROTACs) designed to target HDAC1-3 typically exhibit the selective degradation of HDAC3. Herein, we report cereblon-recruiting PROTACs that degrade HDAC1 with selectivity over HDAC3.
组蛋白去乙酰化酶（HDAC）酶 1-3 存在于几种核心抑制复合物中，是可行的药物靶点。迄今为止，设计用于靶向 HDAC1-3 的蛋白酶体靶向嵌合体（PROTACs）通常表现出对 HDAC3 的选择性降解。在此，我们报告了招募 cereblon 的 PROTACs，其能够选择性地降解 HDAC1，而不是 HDAC3。
Zotero 插件