An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors

作者：Cheng Weiyan; Wang Mixiang; Tian Xin^*; Zhang Xiaojian^*

来源：European Journal of Medicinal Chemistry, 2017, 126: 476-490.

DOI：10.1016/j.ejmech.2016.11.052

• FGFR
• Small molecule inhibitor
• Crystal structure
• DFG-in/out
• Irreversible
• Pharmacological activity

The fibroblast growth factor receptor (FGFR) family receptor tyrosine kinase (RTK) includes four structurally related members, termed as FGFR1, FGFR2, FGFR3, and FGFR4. Given its intimate role in the progression of several solid tumors, excessive FGFR signaling provides an opportunity for anticancer therapy. Along with extensive pharmacological studies validating the therapeutic potential of targeting the FGFRs for cancer treatment, co-crystal structures of FGFRs/inhibitors are continuously coming up to study the mechanism of actions and explore new inhibitors. Herein, we review the reported co-crystals of FGFRs in complex with the corresponding inhibitors, main focusing our attention on the binding models and the pharmacological activities of the inhibitors.

• 出版日期2017-1-27
• 单位南阳医学高等专科学校; 郑州大学