Discovery of a Novel Potent and Orally Efficacious PROTAC Degrader of HPK1 for Tumor Immunotherapy

Hematopoietic progenitor kinase 1 (HPK1), a negative regulator of the TCR signaling pathway, has emerged as an attractive drug target for tumor immunotherapy. Herein, we report the discovery of a series of pyrazine-based HPK1 PROTAC degraders. The representative compound <b>10m</b> demon...

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Autor Principal:	Jun Tong (821940) (author)
Outros autores:	Kaizhen Wang (5139293) (author), Chenyi Liu (21836444) (author), Lin Wang (11986) (author), Qi Miao (552905) (author), Yuxing Wu (3818197) (author), Zhiyi Zhang (279187) (author), Zepeng Liao (21836447) (author), Sheng Jiang (303820) (author), Ruo Wang (2994693) (author), Yibei Xiao (11560194) (author), Kuojun Zhang (10339222) (author)
Publicado:	2025
Subjects:	Biochemistry Medicine Pharmacology Biotechnology Immunology Cancer Infectious Diseases Chemical Sciences not elsewhere classified ≥ 99 %). upon tcr activation two treatment modalities thereby stimulating il tcr signaling pathway superior antitumor effect immunosuppressive effects imposed attractive drug target 0 ± 0 sustained hpk1 degradation max </ sub 50 </ sub 10m </ b >< sub γ release tumor immunotherapy representative compound orally administration novel potent negative regulator molecule therapeutics hpk1 protacs hpk1 ), demonstrated potent degrading hpk1 clinical development 9 nm 1 blockade
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Discovery of a Novel Potent and Orally Efficacious PROTAC Degrader of HPK1 for Tumor Immunotherapy

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