Tyrosine kinase inhibitors bind to overexpressed FGFR2 variants

Stable Identifier
R-HSA-2029992
Type
Reaction [binding]
Species
Homo sapiens
Compartment
plasma membrane, cytosol
ReviewStatus
5/5
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Tyrosine kinase inhibitors bind to overexpressed FGFR2 variants
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Amplified FGFR2 has been shown to be a potential target for a number of ATP-competitive inhibitors, some of which are currently in clinical trials for therapeutic use (Takeda, 2007; Turner, 2010; http://clinicaltrials.gov).
Literature References
PubMed ID Title Journal Year
17505008 AZD2171 shows potent antitumor activity against gastric cancer over-expressing fibroblast growth factor receptor 2/keratinocyte growth factor receptor

Takeda, M, Arao, T, Yokote, H, Komatsu, T, Yanagihara, K, Sasaki, H, Yamada, Y, Tamura, T, Fukuoka, K, Kimura, H, Saijo, N, Nishio, K

Clin Cancer Res 2007
20101236 Integrative molecular profiling of triple negative breast cancers identifies amplicon drivers and potential therapeutic targets

Turner, N, Lambros, MB, Horlings, HM, Pearson, A, Sharpe, R, Natrajan, R, Geyer, FC, van Kouwenhove, M, Kreike, B, Mackay, A, Ashworth, A, van de Vijver, MJ, Reis-Filho, JS

Oncogene 2010
Participants
Input
Output
Participates
as an event of
Functional status

Gain of function of Overexpressed FGFR2 homodimers [plasma membrane]

Disease Entity
Status
Disease
Name Identifier Synonyms
stomach cancer DOID:10534 malignant neoplasm of greater curvature of stomach, unspecified, malignant neoplasm of lesser curvature of stomach, NOS, malignant tumor of body of stomach (disorder), neoplasm of stomach (disorder), Ca lesser curvature - stomach (disorder), malignant neoplasm of greater curve of stomach unspecified (disorder), Ca body - stomach, ca lesser curvature of stomach, ca greater curvature of stomach, malignant neoplasm of lesser curvature of stomach, unspecified, malignant tumor of lesser curve of stomach (disorder), malignant neoplasm of body of stomach, gastric neoplasm, malignant neoplasm of greater curvature of stomach, NOS, Ca body - stomach (disorder), stomach neoplasm, Ca greater curvature - stomach (disorder), malignant neoplasm of lesser curve of stomach unspecified (disorder), malignant tumor of greater curve of stomach (disorder)
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
breast cancer DOID:1612 malignant tumor of the breast, mammary cancer, malignant neoplasm of breast, mammary tumor, primary breast cancer, breast cancer, Ca breast - NOS, breast tumor
Cross References
Mondo
Authored
Rothfels, K  (2012-02-10)
Reviewed
Ezzat, S  (2012-05-15)
Created
Rothfels, K  (2012-01-05)
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