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Eur J Med Chem. 2017 Jan 27;126:476-490. doi: 10.1016/j.ejmech.2016.11.052. Epub 2016 Nov 25.

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

Author information

1
Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China.
2
Department of Pharmacy, The First Affiliated Hospital of Nanyang Medical College, Nanyang 473000, China.
3
Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address: tianx@zzu.edu.cn.
4
Department of Pharmacy, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address: firstpha@163.com.

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.

KEYWORDS:

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

PMID:
27914362
DOI:
10.1016/j.ejmech.2016.11.052
[Indexed for MEDLINE]

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