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PROTAC for Bruton's tyrosine kinase degradation alleviates inflammation in autoimmune diseases.

作者信息

Zhu Can, Yang Zimo, Zhang Yuxiao, Li Zhenjun, Li Guangchen, Yang Bing, Kang Na, Wang Jingwen, Sun Yonghui, Ding Ning, Rao Yu, Liu Wanli

机构信息

State Key Laboratory of Membrane Biology, School of Life Sciences, Tsinghua-Peking Center for Life Sciences, Institute for Immunology, Ministry of Education Key Laboratory of Protein Sciences, Beijing Key Lab for Immunological Research on Chronic Diseases, Beijing Tsinghua Changgeng Hospital, Tsinghua University, Beijing, China.

The First Affiliated Hospital of Anhui Medical University and Institute of Clinical Immunology, Anhui Medical University, Hefei, Anhui, China.

出版信息

Cell Discov. 2024 Aug 6;10(1):82. doi: 10.1038/s41421-024-00711-x.

DOI:10.1038/s41421-024-00711-x
PMID:39107285
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11303405/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b66/11303405/2380f7b09fec/41421_2024_711_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b66/11303405/2380f7b09fec/41421_2024_711_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b66/11303405/2380f7b09fec/41421_2024_711_Fig1_HTML.jpg

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1
PROTAC for Bruton's tyrosine kinase degradation alleviates inflammation in autoimmune diseases.用于降解布鲁顿酪氨酸激酶的PROTAC可减轻自身免疫性疾病中的炎症。
Cell Discov. 2024 Aug 6;10(1):82. doi: 10.1038/s41421-024-00711-x.
2
PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding.PROTAC 介导的布鲁顿酪氨酸激酶降解被共价结合所抑制。
ACS Chem Biol. 2019 Mar 15;14(3):342-347. doi: 10.1021/acschembio.8b01094. Epub 2019 Feb 27.
3
Novel Bruton's tyrosine kinase inhibitor TAS5315 suppresses the progression of inflammation and joint destruction in rodent collagen-induced arthritis.新型布鲁顿酪氨酸激酶抑制剂 TAS5315 抑制啮齿动物胶原诱导性关节炎的炎症进展和关节破坏。
PLoS One. 2023 Feb 23;18(2):e0282117. doi: 10.1371/journal.pone.0282117. eCollection 2023.
4
PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase as a Therapeutic Strategy for Cancer.PROTAC介导的布鲁顿酪氨酸激酶降解作为癌症治疗策略
ACS Med Chem Lett. 2021 Apr 12;12(5):688-689. doi: 10.1021/acsmedchemlett.1c00178. eCollection 2021 May 13.
5
Effect of Bruton's tyrosine kinase inhibitors on platelet aggregation in patients with acute myocardial infarction.布鲁顿酪氨酸激酶抑制剂对急性心肌梗死患者血小板聚集的影响。
Thromb Res. 2019 Jul;179:64-68. doi: 10.1016/j.thromres.2019.04.024. Epub 2019 Apr 24.
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Next-generation Bruton's Tyrosine Kinase (BTK) Inhibitors Potentially Targeting BTK C481S Mutation- Recent Developments and Perspectives.下一代布鲁顿酪氨酸激酶（BTK）抑制剂可能靶向BTK C481S突变——最新进展与展望
Curr Top Med Chem. 2022;22(20):1674-1691. doi: 10.2174/1568026622666220801101706.
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Bruton's Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials.布鲁顿酪氨酸激酶抑制剂（BTKIs）：临床前研究综述与临床试验评估。
Molecules. 2023 Mar 6;28(5):2400. doi: 10.3390/molecules28052400.
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Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.利用PROTAC介导的降解作用靶向布鲁顿酪氨酸激酶中的C481S依鲁替尼耐药突变
Biochemistry. 2018 Jul 3;57(26):3564-3575. doi: 10.1021/acs.biochem.8b00391. Epub 2018 Jun 14.
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Efficacy and safety of Bruton's tyrosine kinase inhibitors in the treatment of pemphigus: A comprehensive literature review and future perspective.布鲁顿酪氨酸激酶抑制剂治疗天疱疮的疗效与安全性：一项全面的文献综述及未来展望
Heliyon. 2023 Nov 27;9(12):e22912. doi: 10.1016/j.heliyon.2023.e22912. eCollection 2023 Dec.
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Inhibitors of Bruton's tyrosine kinase as emerging therapeutic strategy in autoimmune diseases.布鲁顿酪氨酸激酶抑制剂：自身免疫性疾病治疗的新策略
Autoimmun Rev. 2024 May;23(5):103532. doi: 10.1016/j.autrev.2024.103532. Epub 2024 Mar 22.

引用本文的文献

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Advances in precision medicine for lupus nephritis: biomarker- and AI-driven diagnosis and treatment response prediction and targeted therapies.狼疮性肾炎精准医学的进展：生物标志物和人工智能驱动的诊断、治疗反应预测及靶向治疗
EBioMedicine. 2025 Jun 3;117:105785. doi: 10.1016/j.ebiom.2025.105785.
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Razing the scaffolding: the elimination of non-catalytic functions of kinases through targeted protein degradation.拆除脚手架：通过靶向蛋白质降解消除激酶的非催化功能
RSC Med Chem. 2025 Apr 15. doi: 10.1039/d5md00095e.
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BTK inhibitors and next-generation BTK-targeted therapeutics for B-cell malignancies.

本文引用的文献

1
Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127.激酶结构域缺失的 BTK 突变易受临床阶段 BTK 和 IKZF1/3 降解剂 NX-2127 的影响。
Science. 2024 Feb 2;383(6682):eadi5798. doi: 10.1126/science.adi5798.
2
BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies.BTK 抑制剂在血液系统恶性肿瘤和炎症性疾病治疗中的作用机制及临床研究。
J Hematol Oncol. 2022 Oct 1;15(1):138. doi: 10.1186/s13045-022-01353-w.
3
Mechanisms of Resistance to Noncovalent Bruton's Tyrosine Kinase Inhibitors.
用于B细胞恶性肿瘤的布鲁顿酪氨酸激酶（BTK）抑制剂及下一代BTK靶向疗法。
Arch Pharm Res. 2025 May 8. doi: 10.1007/s12272-025-01546-0.
4
Breaking barriers: advancing cellular therapies in autoimmune disease management.突破障碍：推进自身免疫性疾病管理中的细胞疗法。
Front Immunol. 2024 Nov 29;15:1503099. doi: 10.3389/fimmu.2024.1503099. eCollection 2024.
非共价布鲁顿酪氨酸激酶抑制剂耐药机制。
N Engl J Med. 2022 Feb 24;386(8):735-743. doi: 10.1056/NEJMoa2114110.
4
PROTAC targeted protein degraders: the past is prologue.PROTAC 靶向蛋白降解剂：过去是序幕。
Nat Rev Drug Discov. 2022 Mar;21(3):181-200. doi: 10.1038/s41573-021-00371-6. Epub 2022 Jan 18.
5
Pathological inflammation in patients with COVID-19: a key role for monocytes and macrophages.COVID-19 患者的病理性炎症：单核细胞和巨噬细胞的关键作用。
Nat Rev Immunol. 2020 Jun;20(6):355-362. doi: 10.1038/s41577-020-0331-4. Epub 2020 May 6.
6
Systemic lupus erythematosus and diffuse alveolar hemorrhage, etiology and novel treatment strategies.系统性红斑狼疮和弥漫性肺泡出血的病因及新的治疗策略。
Lupus. 2020 Apr;29(4):355-363. doi: 10.1177/0961203320903798. Epub 2020 Feb 9.
7
High-dimensional analysis reveals a pathogenic role of inflammatory monocytes in experimental diffuse alveolar hemorrhage.高维分析揭示了炎症性单核细胞在实验性弥漫性肺泡出血中的致病作用。
JCI Insight. 2019 Aug 8;4(15). doi: 10.1172/jci.insight.129703.
8
Degradation of Bruton's tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas.PROTACs介导布鲁顿酪氨酸激酶突变体的降解用于潜在治疗依鲁替尼耐药的非霍奇金淋巴瘤
Leukemia. 2019 Aug;33(8):2105-2110. doi: 10.1038/s41375-019-0440-x. Epub 2019 Mar 11.
9
PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies.PROTAC诱导的BTK降解作为一种针对突变型BTK C481S诱导的依鲁替尼耐药B细胞恶性肿瘤的新疗法。
Cell Res. 2018 Jul;28(7):779-781. doi: 10.1038/s41422-018-0055-1. Epub 2018 Jun 6.
10
Bruton's Tyrosine Kinase: An Emerging Key Player in Innate Immunity.布鲁顿酪氨酸激酶：先天性免疫中一个新出现的关键角色。
Front Immunol. 2017 Nov 8;8:1454. doi: 10.3389/fimmu.2017.01454. eCollection 2017.