Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases expressed on the cell membrane that play crucial roles in both developmental and adult cells. Dysregulation of FGFRs has been implicated in a wide variety of cancers, such as urothelial carcinoma, hepatocellular car...
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MDPI AG
2019-06-01
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| Series: | Cells |
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| Online Access: | https://www.mdpi.com/2073-4409/8/6/614 |
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| author | Shuyan Dai Zhan Zhou Zhuchu Chen Guangyu Xu Yongheng Chen |
| author_facet | Shuyan Dai Zhan Zhou Zhuchu Chen Guangyu Xu Yongheng Chen |
| author_sort | Shuyan Dai |
| collection | DOAJ |
| description | Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases expressed on the cell membrane that play crucial roles in both developmental and adult cells. Dysregulation of FGFRs has been implicated in a wide variety of cancers, such as urothelial carcinoma, hepatocellular carcinoma, ovarian cancer and lung adenocarcinoma. Due to their functional importance, FGFRs have been considered as promising drug targets for the therapy of various cancers. Multiple small molecule inhibitors targeting this family of kinases have been developed, and some of them are in clinical trials. Furthermore, the pan-FGFR inhibitor erdafitinib (JNJ-42756493) has recently been approved by the U.S. Food and Drug Administration (FDA) for the treatment of metastatic or unresectable urothelial carcinoma (mUC). This review summarizes the structure of FGFR, especially its kinase domain, and the development of small molecule FGFR inhibitors. |
| first_indexed | 2024-03-12T07:53:21Z |
| format | Article |
| id | doaj.art-de5988a879434ba19d1c18fcc93c5ba3 |
| institution | Directory Open Access Journal |
| issn | 2073-4409 |
| language | English |
| last_indexed | 2024-03-12T07:53:21Z |
| publishDate | 2019-06-01 |
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| record_format | Article |
| series | Cells |
| spelling | doaj.art-de5988a879434ba19d1c18fcc93c5ba32023-09-02T20:27:43ZengMDPI AGCells2073-44092019-06-018661410.3390/cells8060614cells8060614Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule InhibitorsShuyan Dai0Zhan Zhou1Zhuchu Chen2Guangyu Xu3Yongheng Chen4NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, ChinaNHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, ChinaNHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, ChinaKey Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education), College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081, Hunan, ChinaNHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, ChinaFibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases expressed on the cell membrane that play crucial roles in both developmental and adult cells. Dysregulation of FGFRs has been implicated in a wide variety of cancers, such as urothelial carcinoma, hepatocellular carcinoma, ovarian cancer and lung adenocarcinoma. Due to their functional importance, FGFRs have been considered as promising drug targets for the therapy of various cancers. Multiple small molecule inhibitors targeting this family of kinases have been developed, and some of them are in clinical trials. Furthermore, the pan-FGFR inhibitor erdafitinib (JNJ-42756493) has recently been approved by the U.S. Food and Drug Administration (FDA) for the treatment of metastatic or unresectable urothelial carcinoma (mUC). This review summarizes the structure of FGFR, especially its kinase domain, and the development of small molecule FGFR inhibitors.https://www.mdpi.com/2073-4409/8/6/614fibroblast growth factor receptorsstructurekinase inhibitortargeted therapy |
| spellingShingle | Shuyan Dai Zhan Zhou Zhuchu Chen Guangyu Xu Yongheng Chen Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors Cells fibroblast growth factor receptors structure kinase inhibitor targeted therapy |
| title | Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors |
| title_full | Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors |
| title_fullStr | Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors |
| title_full_unstemmed | Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors |
| title_short | Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors |
| title_sort | fibroblast growth factor receptors fgfrs structures and small molecule inhibitors |
| topic | fibroblast growth factor receptors structure kinase inhibitor targeted therapy |
| url | https://www.mdpi.com/2073-4409/8/6/614 |
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