Discovery of potent and orally bioavailable degraders of HPK1 based on a novel HPK1 binder

被引:0
|
作者
Zhang, Zhimin
Wu, Mengqiang
Wang, Ling
Yang, Xi
Zhang, Zhiping
Guo, Liubin
Pan, Hao
Zhao, Mengting
Wang, Linli
Liu, Sirui
Dong, Zhao
Jiang, Chunhua
Zheng, Haowen
Liu, Dongzhou
机构
关键词
D O I
10.1158/1538-7445.AM2024-4514
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
4514
引用
收藏
页数:2
相关论文
共 50 条
  • [1] Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1
    Tellis, John C.
    Wei, BinQing
    Siu, Michael
    An, Le
    Chan, Grace Kayan
    Chen, Yong
    Du, Xiangnan
    Gazzard, Lewis
    Hu, Baihua
    Kiefer, James
    Kakiuchi-Kiyota, Satoko
    Lainchbury, Michael
    Linehan, Jonathan L.
    Luo, Xifeng
    Malhotra, Sushant
    Mendonca, Rohan
    Pang, Jodie
    Ran, Yinqing
    Sethuraman, Vijay
    Seward, Eileen
    Sneeringer, Chris
    Su, Dian
    Wang, Weiru
    Wu, Ping
    Moffat, John G.
    Heffron, Timothy P.
    Choo, Edna F.
    Chan, Bryan K.
    ACS MEDICINAL CHEMISTRY LETTERS, 2024, 15 (09): : 1606 - 1614
  • [2] Discovery of novel, potent, selective and orally bioavailable HPK1 inhibitor for enhancing the efficacy of anti-PD-L1 antibody
    Zeng, Shenxin
    Wu, Mingfei
    Jin, Yuyuan
    Ye, Yingqiao
    Xia, Heye
    Chen, Xinyi
    Che, Jinxin
    Wang, Zunyuan
    Wu, Ying
    Dong, Xiaowu
    Chen, Yinqiao
    Huang, Wenhai
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2024, 267
  • [3] Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors
    Ye, Qinda
    Liu, Kai
    Ye, Hai-Fen
    Pan, Jun
    Sokolsky, Alexander
    Wang, Anlai
    Zhang, Ke
    Hummel, Joshua R.
    Kong, Ling
    Behshad, Elham
    He, Xin
    Conlen, Patricia
    Stump, Kristine
    Ye, Min
    Diamond, Sharon
    Covington, Maryanne
    Yeleswaram, Swamy
    Atasoylu, Onur
    Vechorkin, Oleg
    Yao, Wenqing
    ACS MEDICINAL CHEMISTRY LETTERS, 2023, 14 (01): : 5 - 10
  • [4] Discovery of Novel PROTAC-Based HPK1 Degraders with High Potency and Selectivity for Cancer Immunotherapy
    Zhang, Zhimin
    Guo, Liubin
    Zhao, Mengting
    Pan, Hao
    Dong, Zhao
    Wang, Ling
    Yang, Xi
    Zhang, Zhiping
    Wu, Mengqiang
    Chang, Yujie
    Yang, Yacheng
    Sun, Linan
    Liu, Sirui
    Zhu, Rongyao
    Zheng, Haowen
    Dai, Xinyu
    Zhang, Xiaohua
    Jiang, Chunhua
    Zhu, Zhuangzhi
    Zhang, Yuchen
    Liu, Dongzhou
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (21) : 18682 - 18698
  • [5] HPK1 kinase inhibitor: a sufficient approach to target HPK1 to modulate T cell activation in cancer immunotherapy compared with degraders
    Wang, Qin
    Zhu, Xinyi
    Li, Jing
    Xu, Sanjia
    Wang, Ali
    Zhang, Xinwen
    Wang, Xingxing
    Cai, Xiaopeng
    Xing, Haimei
    Liu, Ye
    Liu, Xuesong
    Wang, Zhiwei
    Wang, Lai
    Yuan, Xi
    FRONTIERS IN IMMUNOLOGY, 2025, 16
  • [6] HPK1 as a novel target for cancer immunotherapy
    Sawasdikosol, Sansana
    Zha, Renyuan
    Yang, Boyu
    Burakoff, Steven
    IMMUNOLOGIC RESEARCH, 2012, 54 (1-3) : 262 - 265
  • [7] Discovery of an Exceptionally Orally Bioavailable and Potent HPK1 PROTAC with Enhancement of Antitumor Efficacy of Anti-PD-L1 Therapy
    Wu, Mingfei
    Wu, Yiquan
    Jin, Yuyuan
    Mao, Xinfei
    Zeng, Shenxin
    Yu, Hengyuan
    Zhang, Jingyu
    Jin, Yuheng
    Wu, Yizhe
    Xu, Tengfei
    Chen, Yong
    Wang, Yuwei
    Yao, Xiaojun
    Che, Jinxin
    Huang, Wenhai
    Dong, Xiaowu
    JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (16) : 13852 - 13878
  • [8] Identification of Potent Reverse Indazole Inhibitors for HPK1
    Yu, Elsie C.
    Methot, Joey L.
    Fradera, Xavier
    Lesburg, Charles A.
    Lacey, Brian M.
    Siliphaivanh, Phieng
    Liu, Ping
    Smith, Dustin M.
    Xu, Zangwei
    Piesvaux, Jennifer A.
    Kawamura, Shuhei
    Xu, Haiyan
    Miller, J. Richard
    Bittinger, Mark
    Pasternak, Alexander
    ACS MEDICINAL CHEMISTRY LETTERS, 2021, 12 (03): : 459 - 466
  • [9] HPK1 as a novel target for cancer immunotherapy
    Sansana Sawasdikosol
    Renyuan Zha
    Boyu Yang
    Steven Burakoff
    Immunologic Research, 2012, 54 : 262 - 265
  • [10] Discovery of Novel HPK1 Inhibitors Through Structure-Based Virtual Screening
    Ge, Huizhen
    Peng, Lizeng
    Sun, Zhou
    Liu, Huanxiang
    Shen, Yulin
    Yao, Xiaojun
    FRONTIERS IN PHARMACOLOGY, 2022, 13