FGFR3: A Protein Likely To Be A Drug Target for Cancer (G2261)

Target Name: FGFR3

NCBI ID: G2261

FGFR3

FGFR3: A Protein Likely To Be A Drug Target for Cancer

FGFR3 (FGFR3 variant 2) is a gene that encodes the protein fractional growth factor receptor 3. This gene is a member of the FGFR (Fractional Growth Factor Receptor) family which is a group of transmembrane proteins that are involved in cell signaling. FGFR3 is one of the FGFR variants and is associated with the development and progression of various diseases, including cancer.

The FGFR3 gene was first identified in 2004 and has since been extensively studied. It is located on chromosome 11 and has four exons. The exons are named as Exon 1, Exon 2, Exon 3, and Exon 4. Exon 1 and Exon 2 are the N-terminus and C-terminus of the gene, respectively. Exon 3 and Exon 4 are the middle exons that contain the coding sequence for the FGFR3 protein.

FGFR3 is a protein that consists of 184 amino acid residues. It has a single extracellular domain and a N-terminus that is responsible for the formation of a dimeric complex with the protein PDGF-BB (Platelet-derived growth factor-basic) which is a potent growth factor for various cell types. The N-terminus of FGFR3 contains a unique tryptophan residue (Tyr-21) that is involved in the formation of the dimeric complex.

FGFR3 is a potent receptor for PDGF-BB and has been shown to play a crucial role in the regulation of cell growth, differentiation, and survival. It is involved in the development and maintenance of various tissues, including bones, hearts, kidneys, and digits. It is also involved in the regulation of cell-cell interactions, including the formation of tight junctions and adherens junctions, which are important for tissue structure and function.

In addition to its role in cell signaling, FGFR3 is also a potential drug target. Researchers have identified several potential drug candidates that can inhibit the activity of FGFR3 and have shown that these drugs have the potential to treat various diseases, including cancer. One of the most promising drug candidates is a small molecule inhibitor called FG-197, which is currently being tested in clinical trials for the treatment of various cancers.

Another potential drug target for FGFR3 is a monoclonal antibody (mAb) called FG3-123. This mAb is designed to selectively bind to FGFR3 and can inhibit the activity of FGFR3-expressing cancer cells. FG3-123 has been shown to be effective in preclinical studies and is now being tested in clinical trials for the treatment of various cancers.

In conclusion, FGFR3 is a gene that encodes a protein involved in cell signaling that is associated with the development and progression of various diseases. Its unique tryptophan residue plays a crucial role in the formation of the dimeric complex with PDGF-BB, which is a potent growth factor for various cell types. FGFR3 is also a potential drug target and several drug candidates are currently being developed to inhibit its activity. Further research is needed to understand the full role of FGFR3 in cell signaling and to develop effective treatments for various diseases.

Protein Name: Fibroblast Growth Factor Receptor 3

Functions: Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an essential role in the regulation of chondrocyte differentiation, proliferation and apoptosis, and is required for normal skeleton development. Regulates both osteogenesis and postnatal bone mineralization by osteoblasts. Promotes apoptosis in chondrocytes, but can also promote cancer cell proliferation. Required for normal development of the inner ear. Phosphorylates PLCG1, CBL and FRS2. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Plays a role in the regulation of vitamin D metabolism. Mutations that lead to constitutive kinase activation or impair normal FGFR3 maturation, internalization and degradation lead to aberrant signaling. Over-expressed or constitutively activated FGFR3 promotes activation of PTPN11/SHP2, STAT1, STAT5A and STAT5B. Secreted isoform 3 retains its capacity to bind FGF1 and FGF2 and hence may interfere with FGF signaling

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