FGFR3 mutants bind and are inactivated by tyrosine kinase inhibitors

Stable Identifier
R-HSA-2077420
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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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
15598814 CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma

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

Blood 2005
16091734 FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies

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

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

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

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

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

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

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

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

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

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

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

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

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

Blood 2006
Participants
Participant Of
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created
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