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FGFR3, a member of the fibroblast growth factor receptor family, takes critical roles in cell cycle and angiogenesis processes and especially in cartilage development and homeostasis. The molecular therapeutic strategies for FGFR3 gene-related skeletal dysplasia have been developed for many years. Five major approaches are available for the development of associated treatments, including (1) antagonising downstream FGFR3 signaling, (2) blocking binding between ligands and the FGFR3 receptor, (3) antagonising FGFR3 signaling activities in tyrosine kinases, (4) repurposed drugs for inhibiting FGFR3 signaling, and (5) promoting FGFR3 degradation. Besides, FGFR3 plays a crucial role in some types of cancer, such as breast cancer, glioblastoma, bladder cancer.
Fibroblast growth factor receptor 3 (FGFR3) is also known as cluster of differentiation 333 (CD333), which is encoded by the FGFR3 gene located on chromosome 4, location p16.3. FGFR3 is expressed in cartilage, brain, intestine, and kidneys. FGFR3 is a typical transmembrane protein, which consists of N-terminal extracellular domains containing three Ig-like domains (D1–D3), a transmembrane domain, and an intracellular region harbouring a tyrosine kinase domain.
FGFR3 protein is a tyrosine kinase that has classically been known to play important roles in development, osteogenesis, and bone maintenance. FGFR3 mutations have been described in spermatocytic seminoma, multiple myeloma and cervical cancer. FGFR3 ia regulated by several signaling pathways, including antagonising the MAPK signalling pathways; interfering with ligand-dependent binding; TKIs inhibit the activities of tyrosine kinases; meclozine inhibits the MAPK signalling pathway by blocking ERK1/2 phosphorylation; FGFR3 negatively mediates function of PTH/PTHrP-PTH1R signalling via JAK/STA T or IHH-PTHrP signalling pathways; HDAC6 or statins may be involved in promoting degradation of FGFR3, snail1 simultaneously regulates the MAPK and STA T1 pathways in the proliferation and differentiation of chondrocytes.
The FGFR3 is a negative regulator of chondrogenesis, which plays an important role in cartilage development and homeostasis. FGFR3 negatively regulates chondrocyte proliferation and differentiation by activating downstream signaling pathways to maintain reconstructive balance in the growth plate. Gain-of-function mutations result in constitutively activated FGFR3, leading to aberrant signal transduction, and accounting for inhibition of chondrocyte proliferation and differentiation. FGFR3 is expressed in chondrocytes and osteoblasts, whose mutations are associated with bone growth disorders such as achondroplasia, chondrodysplasia, and thanatophoric dysplasia.
FGFR3 is a prognostic and predictive biomarker in urothelial bladder cancer. FGFR3 mRNA is overexpressed in urothelial tumors, which is associated with tumor invasiveness, proliferation, and motility. FGFR3 gene mutations, amplifications, and fusions are associated with luminal-papillary subtype of urothelial cancer. Besides, the alterations of FGFR3 gene are associated with less favorable outcomes in the context of chemotherapy for advanced disease. Some studies have suggested that FGFR3 takes a crucial part in regulating the innate immune system, including inhibition of interferons and stimulation of tumor necrosis factor-α.
Approved Drugs
Pazopanib, nintedanib, ponatinib, lenvatinib, fostamatinib, etc.
Drugs in Development
XL999, etc.
Protein Tyrosine Kinase Activity
Pazopanib, nintedanib, ponatinib, lenvatinib, etc.
hyperphosphatemia, stomatitis, diarrhea, elevated creatinine, fatigue, hand-food syndrome, decreased appetite, elevated liver enzymes and significant gastrointestinal effects, embryo-fetal mortality, or developmental abnormalities.
FGFR3 TestingCD BioSciences provides FGFR3 testing services by Elisa, WB, IP, IHC or IF assay. The results of FGFR3 testing are used to evaluate the activities of candidates against FGFR3 or targeted diseases. You can choose one or more testing ways to detect the level of FGFR3 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
Cancer 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 cancer model according to your requirements to evaluate the inhibitory activity of your candidates targeted FGFR3. 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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