FGFR3 mutants bind and are inactivated by tyrosine kinase inhibitors

Stable Identifier
Reaction [binding]
Homo sapiens
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FGFR3 has been shown to be a target of a range of different tyrosine kinase inhibitors, including those restricted to in vitro use as well as a number that are currently in clinical trials for therapeutic use (see for instance, Paterson, 2004; Trudel, 2004; Trudel, 2005; Grand, 2004, Chen, 2005; Bernard-Pierrot, 2006; http::/clinicaltrials.gov). There are also two anti-FGFR3 antibodies that have shown preliminary promise in cancer cell lines or mouse models (Qing, 2009; Trudel, 2006).

Literature References
PubMed ID Title Journal Year
16091734 FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies

Gilliland, DG, Cohen, S, Huntly, BJ, Griffin, J, Duclos, N, Fabbro, D, Okabe, R, Moore, S, Mitsiades, CS, Lee, BH, Chen, J, Kutok, J, Adelsperger, J, Anderson, KC, Coburn, A, Williams, I

Oncogene 2005
15598814 CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma

Wei, E, Wiesmann, M, Trudel, S, Chang, H, Chen, C, Stewart, AK, Li, ZH, Heise, C, Reece, D

Blood 2005
14871245 Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma

Trudel, S, Pollett, JB, Wen, XY, Paterson, JL, Masih-Khan, E, Chang, H, Stewart, AK, Li, Z

Br J Haematol 2004
19381019 Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice

Stephan, JP, Dornan, D, Stinson, S, Wiesmann, C, Du, X, Wu, P, Qing, J, Ashkenazi, A, Wu, Y, Tien, J, French, D, Totpal, K, Chan, P, Chen, Y, Marsters, S, Ross, S, Li, H, Wang, QR, Stawicki, S

J Clin Invest 2009
18757432 Characterization of the recurrent 8p11-12 amplicon identifies PPAPDC1B, a phosphatase protein, as a new therapeutic target in breast cancer

Delattre, O, Pierron, G, Reyal, F, Stransky, N, Bernard-Pierrot, I, Radvanyi, F, Vallot, C, Gruel, N, Raynal, V, Vincent-Salomon, A

Cancer Res 2008
14715624 Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma

Trudel, S, Chesi, M, Bergsagel, PL, Farooqi, Y, Affer, M, Robbiani, DF, Ely, S

Blood 2004
15029211 Targeting FGFR3 in multiple myeloma: inhibition of t(4;14)-positive cells by SU5402 and PD173074

Rahemtulla, A, Grand, EK, Chase, AJ, Cross, NC, Heath, C

Leukemia 2004
16467200 The inhibitory anti-FGFR3 antibody, PRO-001, is cytotoxic to t(4;14) multiple myeloma cells

Wei, E, Yayon, A, Trudel, S, Rom, E, Chumakov, I, Chang, H, Li, ZH, Stewart, AK, Liang, SB, Singer, Y, Kotzer, S

Blood 2006
Functional status

Gain of function of FGFR3 mutant dimers [plasma membrane]

Disease Entity
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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