Structure-based design of a dual-warhead covalent inhibitor of FGFR4
oleh: Xiaojuan Chen, Huiliang Li, Qianmeng Lin, Shuyan Dai, Sitong Yue, Lingzhi Qu, Maoyu Li, Ming Guo, Hudie Wei, Jun Li, Longying Jiang, Guangyu Xu, Yongheng Chen
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2022-03-01 |
Deskripsi
Fibroblast growth factor receptor 4 (FGFR4) is a promising target for the treatment of hepatocellular carcinoma, but current FGFR4 covalent inhibitors target only one of the two cysteine residues (Cys477 or Cys552) that provide FGFR4-specificity. Here, a dual-warhead covalent FGFR4 inhibitor that can covalently target both cysteine residues of FGFR4 is reported, and strong selectivity for FGFR4 is observed.