Kinase Atlas

Function: 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.

Site	Maximum Consensus Site Population	Minimum Consensus Site Population	Median Consensus Site Population
MPP	20	11	15.5
DRS	2	2	2.0
ATP	15	4	9.5

PDB ID	Maximum Consensus Site Population
PDB ID	MPP site	DFG site	PIF site	DRS site	DEF site	EDI site	MT3 site	AAS site	LBP site	CMP site	PDIG site	ATP site	PMP site
Total Druggable Structures per Site	1	0	0	0	0	0	0	0	0	0	0	0	0
4K33	20	0	0	2	0	0	0	0	0	0	0	15	0
AFP22607	0	0	0	0	0	0	0	0	0	0	0	0	0

P22607