Related Experiment Video
Updated: Jul 4, 2026
09:38
Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
Published on: August 11, 2017
Drug-sensitive FGFR2 mutations in endometrial carcinoma
Amit Dutt1, Helga B Salvesen, Tzu-Hsiu Chen
1Department of Medical Oncology and Center for Cancer Genome Discovery, Dana-Farber Cancer Institute, Boston, MA 02115, USA.
Summary
Somatic mutations in the fibroblast growth factor receptor 2 (FGFR2) gene drive cancer in 12% of endometrial carcinomas. Inhibiting FGFR2 kinase activity offers a potential new therapy for these cancers.
Area of Science:
- Oncology
- Molecular Biology
- Genetics
Background:
- Tyrosine kinase activation is a key driver in many cancers.
- Fibroblast growth factor receptor 2 (FGFR2) is a druggable target for cancer therapy.
Purpose of the Study:
- To investigate the role of fibroblast growth factor receptor 2 (FGFR2) gene mutations in endometrial carcinoma.
- To assess the therapeutic potential of targeting FGFR2 in endometrial cancer.
Main Methods:
- Somatic mutation analysis of the FGFR2 gene in endometrial carcinoma samples.
- Functional studies involving ectopic expression of mutated FGFR2 in NIH 3T3 cells.
- Inhibition of FGFR2 kinase activity in cancer cell lines.
Main Results:
- FGFR2 mutations were identified in 12% of endometrial carcinomas, and also found in lung squamous cell and cervical carcinomas.
- Identified FGFR2 mutations are constitutively activated and oncogenic.
- Inhibition of FGFR2 kinase activity suppressed transformation and survival in endometrial carcinoma cells with FGFR2 mutations.
Conclusions:
- FGFR2 is a novel therapeutic target in endometrial carcinoma.
- FGFR2 mutations, some linked to developmental disorders, play a significant role in endometrial carcinogenesis.
Related Concept Videos
01:11Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
02:38Mitogens and the Cell Cycle
Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...