机构：[1]East China Normal Univ, Inst Biomed Sci, Shanghai Frontiers Sci Ctr Genome Editing & Cell T, Shanghai Key Lab Regulatory Biol, Shanghai 200241, Peoples R China[2]East China Normal Univ, Sch Life Sci, Shanghai 200241, Peoples R China[3]Guangzhou Univ Chinese Med, Clin Med Coll 2, State Key Lab Dampness Syndrome Chinese Med, Guangzhou 510006, Peoples R China广东省中医院
B-cell lymphoma 6 (BCL6) is a transcriptional repressor that regulates the differentiation of B lymphocytes and mediates the formation of germinal centers (GCs) by recruiting corepressors through the BTB domain of BCL6. Physiological processes regulated by BCL6 involve cell activation, differentiation, DNA damage, and apoptosis. BCL6 is highly expressed when the gene is mutated, leading to the malignant proliferation of cells and drives tumorigenesis. BCL6 overexpression is closely correlated with tumorigenesis in diffuse large B-cell lymphoma (DLBCL) and other lymphomas, and BCL6 inhibitors can effectively inhibit some lymphomas and overcome resistance. Therefore, targeting BCL6 might be a promising therapeutic strategy for treating lymphomas. Herein, we comprehensively review the latest development of BCL6 inhibitors in diffuse large B-cell lymphoma and discuss the overview of the pharmacophores of BCL6 inhibitors and their efficacies in vitro and in vivo. Additionally, the current advances in BCL6 degraders are provided.
基金：
National Natural Science Foundation of China; Natural Science Foundation of Guangdong Province; [82160461]; [2022A1515010103]
第一作者机构：[1]East China Normal Univ, Inst Biomed Sci, Shanghai Frontiers Sci Ctr Genome Editing & Cell T, Shanghai Key Lab Regulatory Biol, Shanghai 200241, Peoples R China[2]East China Normal Univ, Sch Life Sci, Shanghai 200241, Peoples R China
共同第一作者：
通讯作者：
通讯机构：[1]East China Normal Univ, Inst Biomed Sci, Shanghai Frontiers Sci Ctr Genome Editing & Cell T, Shanghai Key Lab Regulatory Biol, Shanghai 200241, Peoples R China[2]East China Normal Univ, Sch Life Sci, Shanghai 200241, Peoples R China
推荐引用方式(GB/T 7714)：
Gu Haijun,He Jia,Li Yuzhan,et al.B-cell Lymphoma 6 Inhibitors: Current Advances and Prospects of Drug Development for Diffuse Large B-cell Lymphomas[J].JOURNAL OF MEDICINAL CHEMISTRY.2022,65(23):15559-15583.doi:10.1021/acs.jmedchem.2c01433.
APA：
Gu, Haijun,He, Jia,Li, Yuzhan,Mi, Dazhao,Guan, Tian...&Chen, Yihua.(2022).B-cell Lymphoma 6 Inhibitors: Current Advances and Prospects of Drug Development for Diffuse Large B-cell Lymphomas.JOURNAL OF MEDICINAL CHEMISTRY,65,(23)
MLA：
Gu, Haijun,et al."B-cell Lymphoma 6 Inhibitors: Current Advances and Prospects of Drug Development for Diffuse Large B-cell Lymphomas".JOURNAL OF MEDICINAL CHEMISTRY 65..23(2022):15559-15583
医学