BCL6公司
化学
淋巴瘤
生发中心
癌变
弥漫性大B细胞淋巴瘤
癌症研究
细胞生长
B细胞
生物
基因
免疫学
生物化学
抗体
作者
Haijun Gu,Jiaxun He,Yuzhan Li,Dazhao Mi,Tian Guan,Weikai Guo,Bo Liu,Yi Hua Chen
标识
DOI:10.1021/acs.jmedchem.2c01433
摘要
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.
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