Novel Regulatory Factors and Small-Molecule Inhibitors of FGFR4 in Cancer

被引:13
作者
Liu, Yanan [1 ,2 ]
Wang, Canwei [1 ]
Li, Jifa [1 ]
Zhu, Jiandong [1 ]
Zhao, Chengguang [1 ,2 ]
Xu, Huanhai [1 ]
机构
[1] Wenzhou Med Univ, Affiliated Yueqing Hosp, Wenzhou, Peoples R China
[2] Wenzhou Med Univ, Sch Pharmaceut Sci, Wenzhou, Peoples R China
关键词
FGFR4; FGF19; cancer; activator; inhibitor;
D O I
10.3389/fphar.2021.633453
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Fibroblast growth factor receptor 4 (FGFR4) is a tyrosine kinase receptor that is a member of the fibroblast growth factor receptor family and is stimulated by highly regulated ligand binding. Excessive expression of the receptor and its ligand, especially FGF19, occurs in many types of cancer. Abnormal FGFR4 production explains these cancer formations, and therefore, this receptor has emerged as a potential target for inhibiting cancer development. This review discusses the diverse mechanisms of oncogenic activation of FGFR4 and highlights some currently available inhibitors targeting FGFR4.
引用
收藏
页数:10
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共 87 条
[1]   Fibroblast growth factor receptor 4 induced resistance to radiation therapy in colorectal cancer [J].
Ahmed, Mohamed A. ;
Selzer, Edgar ;
Doerr, Wolfgang ;
Jomrich, Gerd ;
Harpain, Felix ;
Silberhumer, Gerd R. ;
Muellauer, Leonhard ;
Holzmann, Klaus ;
Grasl-Kraupp, Bettina ;
Grusch, Michael ;
Berger, Walter ;
Marian, Brigitte .
ONCOTARGET, 2016, 7 (43) :69976-69990
[2]   Rationale for targeting fibroblast growth factor receptor signaling in breast cancer [J].
Andre, Fabrice ;
Cortes, Javier .
BREAST CANCER RESEARCH AND TREATMENT, 2015, 150 (01) :1-8
[3]   Targeting FGFR with Dovitinib (TKI258): Preclinical and Clinical Data in Breast Cancer [J].
Andre, Fabrice ;
Bachelot, Thomas ;
Campone, Mario ;
Dalenc, Florence ;
Perez-Garcia, Jose M. ;
Hurvitz, Sara A. ;
Turner, Nicholas ;
Rugo, Hope ;
Smith, John W. ;
Deudon, Stephanie ;
Shi, Michael ;
Zhang, Yong ;
Kay, Andrea ;
Porta, Diana Graus ;
Yovine, Alejandro ;
Baselga, Jose .
CLINICAL CANCER RESEARCH, 2013, 19 (13) :3693-3702
[4]   Advances and challenges in targeting FGFR signalling in cancer [J].
Babina, Irina S. ;
Turner, Nicholas C. .
NATURE REVIEWS CANCER, 2017, 17 (05) :318-332
[5]   Sp3 controls fibroblast growth factor receptor 4 gene activity during myogenic differentiation [J].
Cavanaugh, Eric ;
DiMario, Joseph X. .
GENE, 2017, 617 :24-31
[6]  
Chen SM, 2016, AM J TRANSL RES, V8, P3309
[7]   Functional FGFR4 Gly388Arg polymorphism contributes to oral squamous cell carcinoma susceptibility [J].
Chou, Chia-Hsuan ;
Hsieh, Ming-Ju ;
Chuang, Chun-Yi ;
Lin, Jen-Tsun ;
Yeh, Chia-Ming ;
Tseng, Pao-Yu ;
Yang, Shun-Fa ;
Chen, Mu-Kuan ;
Lin, Chiao-Wen .
ONCOTARGET, 2017, 8 (56) :96225-96238
[8]   Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors [J].
Dai, Shuyan ;
Zhou, Zhan ;
Chen, Zhuchu ;
Xu, Guangyu ;
Chen, Yongheng .
CELLS, 2019, 8 (06)
[9]   Targeting FGF19 inhibits tumor growth in colon cancer xenograft and FGF19 transgenic hepatocellular carcinoma models [J].
Desnoyers, Lr ;
Pai, R. ;
Ferrando, Re ;
Hotzel, K. ;
Le, T. ;
Ross, J. ;
Carano, R. ;
D'Souza, A. ;
Qing, J. ;
Mohtashemi, I. ;
Ashkenazi, A. ;
French, Dm .
ONCOGENE, 2008, 27 (01) :85-97
[10]   Interleukin-1 in the pathogenesis and treatment of inflammatory diseases [J].
Dinarello, Charles A. .
BLOOD, 2011, 117 (14) :3720-3732