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FGFR2 is a member of the fibroblast growth factor receptor family, which has important roles in embryonic development and tissue repair, especially bone and blood vessels. Studies indicated that mutations of FGFR2 are associated with numerous medical conditions that include abnormal bone development (e.g., craniosynostosis syndromes) and cancer. It is associated with prostate cancer, gastric cancer, Beare-Stevenson cutis gyrata syndrome, Jackson-Weiss syndrome, and others.
Fibroblast growth factor receptor 2 (FGFR2), is also known as cluster of differentiation 332 (CD332). It is a protein encoded by the FGFR2 gene residing on chromosome 10. Just as the other members of the fibroblast growth factor receptor family, FGFR2 signals through bound to its ligand and dimerization (pairing of receptors), which initiates a cascade of intracellular signals (involving in cell division, growth, and differentiation) by tyrosine kinase domains.
FGFR2 exhibited important activities on embryonic development and tissue repair, especially bone and blood vessels. Like FGFR1, FGFR2 has two naturally occurring isoforms, FGFR2IIIb and FGFR2IIIc. They are created by splicing of the third immunoglobulin-like domain. FGFR2IIIb is predominantly found in ectoderm derived tissues and endothelial organ lining, i.e., skin and internal organs, and FGFR2IIIc is found in mesenchyme, which includes craniofacial bone and for this reason the mutations of this gene and isoform are associated with craniosynostosis.
Fibroblast growth factor receptor 2 (FGFR2) is a receptor tyrosine kinase that induces proliferation and migration. FGFR2 mutations may result in premature suture fusion through upregulation of epidermal growth factor (EGF) and platelet derived growth factor (PDGF) α signaling. Beare-Stevenson cutis gyrata syndrome is characterized by several anomalies in addition to the skin condition of redundant and convoluted folds, including craniosynostosis, ear defects, anogenital anomalies. Clinical researches indicated that Beare-Stevenson is caused by de novo heterozygous mutations in FGFR2, including Tyr375Cys mutation in the transmembrane domain, and Ser372Cys mutation in the carboxy-terminal end of the linker region between IgIII and transmembrane domains. Moreover, FGFR2 has ability to regulate bone formation within the nucleolus.
FGF2 promotes cell proliferation, prevents cell death, and increases tumor angiogenesis. FGF2 always expresses in tumor, such as prostate cancer, which is crucial in the initiation, progression, and particularly metastasis of prostate cancer. Researches revealed that Ablation of FGF2 alleles in TRAMP mice significantly inhibits the progression to poorly differentiated prostatic tumors, decreases metastasis to other organs, and increases the lifespan of the mice.
Approved Drugs
Palifermin, regorafenib, nintedanib, foreskin fibroblast, foreskin keratinocyte, etc.
Drugs in Development
Sucrosofate, 4-[4-(1-Amino-1-Methylethyl)Phenyl]-5-Chloro-N-[4-(2-Morpholin-4-Ylethyl)Phenyl]Pyrimidin-2-Amine, etc.
Protein Tyrosine Kinase Activity
Palifermin, regorafenib, nintedanib, foreskin fibroblast, foreskin keratinocyte, etc.
Asthenia/fatigue, HFSR, diarrhea, decreased appetite/food intake, hypertension, mucositis, dysphonia, and infection, pain (not otherwise specified), decreased weight, gastrointestinal and abdominal pain, rash, fever, infection, cellulitis, osteomyelitis, and nausea.
FGFR2 Testing ServicesCD BioSciences provides FGFR2 testing services by Elisa, WB, IP, IHC or IF assay. The results of FGFR2 testing are used to evaluate the activities of candidates against FGFR2 or targeted diseases. You can choose one or more testing ways to detect the level of FGFR2 according to your experiment.
Hit Identification (show more)The goal of early drug discovery is to find novel lead compounds that have the desired potency, selectivity, and ADMET properties for pre-clinical evaluation.
CD BioSciences offers hit identification services to make your find targeted compounds more successful and faster.
Pharmacological Experiments (show more)We will make a specific experimental plan according to your requirements, including but not limited to
Disease Models Screening (show more)We will make specific disease models to accelerate your targeted drug discovery project, including but not limited to
CD BioSciences will establish the specific disease model according to your requirements to evaluate the inhibitory activity of your candidates targeted FGFR2. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.
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