Citation: Yifan Feng, Chengjuan Chen, Anqi Shao, Qingyang Zhang, Lan Sun, Hai-Yu Hu, Tiantai Zhang. Recent advances in interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors and PROTACs[J]. Chinese Chemical Letters, ;2025, 36(12): 110963. doi: 10.1016/j.cclet.2025.110963 shu

Recent advances in interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors and PROTACs

Yifan Feng ^{a, 1} ,
Chengjuan Chen ^{a, 1} ,
Anqi Shao ^b ,
Qingyang Zhang ^a ,
Lan Sun ^{a, *,} ,
Hai-Yu Hu ^{a, *,} ,
Tiantai Zhang ^{a, *,}

a.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
b.
Department of Dermatology, Vagelos College of Physicians and Surgeons, Columbia University Irving Medical Center, New York 10032, United States

sunhanxing2005@imm.ac.cn

haiyu.hu@imm.ac.cn

ttzhang@imm.ac.cn

Received Date: 2 December 2024
Revised Date: 14 February 2025
Accepted Date: 17 February 2025
Available Online: 17 February 2025

Figures(23)

Interleukin-1 receptor-associated kinase 4 (IRAK4) is a key kinase downstream of the interleukin-1 receptor (IL-1R) and Toll-like receptors (TLRs) signaling pathway, whose overexpression and hyperactivation have been associated with several inflammatory diseases or cancer. Therefore, targeting IRAK4 has emerged as a promising therapeutic strategy. A range of potent and selective IRAK4 inhibitors and degraders based on draggability have been designed and developed. This article provides a comprehensive summary of the IRAK4 inhibitors and degraders that have been developed and discusses the challenges and opportunities for research in this area.
- Interleukin-1 receptor-associated kinase 4,
- IL-1R/TLRs signal pathway,
- Inflammatory/autoimmune diseases,
- IRAK4 inhibitors,
- IRAK4 PROTACs
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沈阳化工大学材料科学与工程学院沈阳 110142