PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies.
作者信息
Sun Yonghui, Zhao Xingwang, Ding Ning, Gao Hongying, Wu Yue, Yang Yiqing, Zhao Meng, Hwang Jinseok, Song Yuqin, Liu Wanli, Rao Yu
机构信息
MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology, Tsinghua University, Beijing, 100084, China.
MOE Key Laboratory of Protein Sciences, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, School of Life Sciences, Beijing Key Lab for Immunological Research on Chronic Diseases, Tsinghua University, Beijing, 100084, China.
出版信息
Cell Res. 2018 Jul;28(7):779-781. doi: 10.1038/s41422-018-0055-1. Epub 2018 Jun 6.
Abstract
摘要
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本文引用的文献
1
BTK drives ibrutinib resistance via ERK1/2 and protects BTK MYD88-mutated cells by a paracrine mechanism.BTK 通过 ERK1/2 驱动伊布替尼耐药，并通过旁分泌机制保护 BTK MYD88 突变细胞。
Blood. 2018 May 3;131(18):2047-2059. doi: 10.1182/blood-2017-10-811752. Epub 2018 Mar 1.
2
Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.阿卡替尼（ACP-196）用于复发的慢性淋巴细胞白血病
N Engl J Med. 2016 Jan 28;374(4):323-32. doi: 10.1056/NEJMoa1509981. Epub 2015 Dec 7.
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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.劫持E3泛素连接酶大脑神经酰胺酶以有效靶向BRD4。
Chem Biol. 2015 Jun 18;22(6):755-63. doi: 10.1016/j.chembiol.2015.05.009. Epub 2015 Jun 4.
4
DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation.药物研发。邻苯二甲酰亚胺缀合作为体内靶蛋白降解的一种策略。
Science. 2015 Jun 19;348(6241):1376-81. doi: 10.1126/science.aab1433. Epub 2015 May 21.
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Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib.伊布替尼的布鲁顿酪氨酸激酶抑制剂耐药机制。
N Engl J Med. 2014 Jun 12;370(24):2286-94. doi: 10.1056/NEJMoa1400029. Epub 2014 May 28.
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Ibrutinib resistance in chronic lymphocytic leukemia.慢性淋巴细胞白血病中的依鲁替尼耐药性。
N Engl J Med. 2014 Jun 12;370(24):2352-4. doi: 10.1056/NEJMc1402716. Epub 2014 May 28.
7
The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy.布鲁顿酪氨酸激酶抑制剂 PCI-32765 可阻断 B 细胞激活，并在自身免疫性疾病和 B 细胞恶性肿瘤模型中有效。
Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. doi: 10.1073/pnas.1004594107. Epub 2010 Jul 6.
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Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma.弥漫性大 B 细胞淋巴瘤中慢性活性 B 细胞受体信号转导。
Nature. 2010 Jan 7;463(7277):88-92. doi: 10.1038/nature08638.
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Bruton's tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain.布鲁顿酪氨酸激酶（Btk）：功能、调控及转化，特别强调PH结构域
Immunol Rev. 2009 Mar;228(1):58-73. doi: 10.1111/j.1600-065X.2008.00741.x.
10
Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase.布鲁顿酪氨酸激酶选择性不可逆抑制剂的发现。
ChemMedChem. 2007 Jan;2(1):58-61. doi: 10.1002/cmdc.200600221.
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