title: An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.
abstract: 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.
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China.
authors.forename: Weiyan
authors.initials: W
authors.lastname: Cheng
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Nanyang Medical College, Nanyang 473000, China.
authors.forename: Mixiang
authors.initials: M
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address: tianx@zzu.edu.cn.
authors.forename: Xin
authors.initials: X
authors.lastname: Tian
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address: firstpha@163.com.
authors.forename: Xiaojian
authors.initials: X
authors.lastname: Zhang
mesh_terms: D006801:Humans; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D020794:Receptor Protein-Tyrosine Kinases / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D047428:Protein Kinase Inhibitors; D054852:Small Molecule Libraries; D020794:Receptor Protein-Tyrosine Kinases
keywords: Crystal structure; DFG-in/out; FGFR; Irreversible; Pharmacological activity; Small molecule inhibitor