PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
Dear Editor,Non-Hodgkin”s lymphoma (NHL) is a type of cancer that mainly develops from B-cell malignancies, causing 231,400 deaths in 2015 globally. According to the American Cancer Society, around 66,000 new cases of NHL are diagnosed each year in the United States.1 Bruton”s tyrosine kinase (BTK) is an enzyme encoded by the BTK gene in human. BTK is expressed in all cell lineages of the hematopoietic system except for T cells.2 As a cytoplasmic tyrosine kinase of the TEC family, BTK plays a crucial role in B cell development, differentiation, and signaling. BTK is closely associated with chronic B-cell receptor (BCR) activation, and is critical for the survival of B-cell neoplasms.3
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the National Natural Science Foundation of China#81573277, 81622042, 81773567;National Major Scientific and Technological Special Project for ”Significant New Drugs Development”#SQ2017ZX095003;Tsinghua University Initiative Scientific Research Program. This work was also financially supported by the NSFC81670187;Beijing Natural Science Foundation No. 7172047. We thank Prof. Haitao Li and Prof. Qinghua Tao of Tsinghua University for helpful discussions
2018-10-10（万方平台首次上网日期，不代表论文的发表时间）
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