文献类型：期刊文献

中文题名：Rifamycin O as a novel CRBN ligand for targeted degradation of IKZF1/3 proteins in hematopoietic malignancies

作者：Liang Liao[1,2];Qiang Wang[1];Zhengyang Gao[1];Jiayao Liu[1];Yuxuan Tong[1];Xin Chen[1];Jin Zhu[1];Jian Li[1,3,4];Jinlian Wei[1]

机构：[1]State Key Laboratory of Bioreactor Engineering,Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism,Frontiers Science Center for Materiobiology and Dynamic Chemistry,Shanghai Key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China;[2]Department of Technology Transfer,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China;[3]Key Laboratory of Xinjiang Phytomedicine Resource and Utilization,Ministry of Education,School of Pharmacy,Shihezi University,Shihezi 832003,China;[4]Key Laboratory of Tropical Biological Resources of Ministry of Education,College of Pharmacy,Hainan University,Haikou 570228,China

年份：2026

卷号：16

期号：1

起止页码：647

中文期刊名：Acta Pharmaceutica Sinica B

外文期刊名：药学学报(英文版)

基金：supported by the National Natural Science Foundation of China(22037002,32121005);Innovative Research Team of High-level Local Universities in Shanghai(SHSMU-ZDCX20212702,China);National Special Fund for State Key Laboratory of Bioreactor Engineering(2060204,China);Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism(2021 Sci&Tech 03-28,China).

语种：英文

中文关键词：CRBN;Fluorescence polarization;Rifamycin O;Novel ligand;Hematopoietic malignancies;IKZF1/3;Molecular glue;Proteasomal degradation

摘要：To the Editor:Cereblon(CRBN)has emerged as a promising therapeutic target,enabling the design of proteolysis-targeting chimeras(PROTACs)and molecular glues(MGs)for targeted protein degradation1.The immunomodulatory imide drugs(IMiDs),such as thalidomide,lenalidomide and pomalidomide,represent classical CRBN ligands and have been widely used in the treatment of hematopoietic malignancies.These IMiDs exert their immunomodulatory and anti-inflammatory effects by binding to CRBN and triggering the degradation of neosubstrates,including IKZF1 and IKZF3,which are crucial for B and T cells biology2.