Covpdb











Protein
Protein Name Fibroblast growth factor receptor 4
#PDB ID 14
Organism Homo sapiens (Human)
Uniprot ID/ACC P22455 (FGFR4_HUMAN)
Synonym(s)
  •   hydroxyaryl-protein kinase
  • protein-tyrosine kinase
  • tyrosine kinase related to fibroblast growth factor receptor
  • tyrosylprotein kinase
  • CD334
  • JTK2
  • TKF
show 6 synonym(s)
Gene Symbol FGFR4
Gene ID 2264
Sequence MRLLLALLGVLLSVPGPPVLSLEASEEVELEPCLAPSLEQQEQELTVALGQPVRLCCGRAERGGHWYKEGSRLAPAGRVRGWRGRLEIASFLPEDAGRYLCLARGSMIVLQNLTLITGDSLTSSNDDEDPKSHRDPSNRHSYPQQAPYWTHPQRMEKKLHAVPAGNTVKFRCPAAGNPTPTIRWLKDGQAFHGENRIGGIRLRHQHWSLVMESVVPSDRGTYTCLVENAVGSIRYNYLLDVLERSPHRPILQAGLPANTTAVVGSDVELLCKVYSDAQPHIQWLKHIVINGSSFGADGFPYVQVLKTADINSSEVEVLYLRNVSAEDAGEYTCLAGNSIGLSYQSAWLTVLPEEDPTWTAAAPEARYTDIILYASGSLALAVLLLLAGLYRGQALHGRHPRPPATVQKLSRFPLARQFSLESGSSGKSSSSLVRGVRLSSSGPALLAGLVSLDLPLDPLWEFPRDRLVLGKPLGEGCFGQVVRAEAFGMDPARPDQASTVAVKMLKDNASDKDLADLVSEMEVMKLIGRHKNIINLLGVCTQEGPLYVIVECAAKGNLREFLRARRPPGPDLSPDGPRSSEGPLSFPVLVSCAYQVARGMQYLESRKCIHRDLAARNVLVTEDNVMKIADFGLARGVHHIDYYKKTSNGRLPVKWMAPEALFDRVYTHQSDVWSFGILLWEIFTLGGSPYPGIPVEELFSLLREGHRMDRPPHCPPELYGLMRECWHAAPSQRPTFKQLVEALDKVLLAVSEEYLDLRLTFGPYSPSGGDASSTCSSSDSVFSHDPLPLGSSSFPFGSGVQT
Protein Class TRANSFERASE
Function Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation of lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism and phosphate homeostasis. Required for normal down-regulation of the expression of CYP7A1, the rate-limiting enzyme in bile acid synthesis, in response to FGF19. Phosphorylates PLCG1 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. Promotes SRC-dependent phosphorylation of the matrix protease MMP14 and its lysosomal degradation. FGFR4 signaling is down-regulated by receptor internalization and degradation; MMP14 promotes internalization and degradation of FGFR4. Mutations that lead to constitutive kinase activation or impair normal FGFR4 inactivation lead to aberrant signaling.
Bound Ligands
Ligand ID HET Code PDB ID Binding Affinity Binding Database Structure Complex Card
COVPDB178 37O 4QQ5 IC50 : 482 nM PDBBind SHOW
COVPDB178 37O 4QQC IC50 : 45.3 nM PDBBind SHOW
COVPDB211 40M 4XCU Kd : 6 nM PDBBind SHOW
COVPDB430 99K 5NUD Kd : 32 nM PDBBind SHOW
COVPDB433 9CT 5NWZ Kd : 0.8 nM PDBBind SHOW
COVPDB798 FI3 4R6V IC50 : 35.3 nM PDBBind SHOW
COVPDB1266 QS7 6V9C IC50 : 100 nM, IC50 : 500 nM BindingDB SHOW
COVPDB514 AWX 6IUO
-
-
SHOW
COVPDB595 BYU 6JPE
-
-
SHOW
COVPDB1466 XL8 6NVG
-
-
SHOW
COVPDB1464 XL6 6NVH
-
-
SHOW
COVPDB1463 XL5 6NVJ
-
-
SHOW
COVPDB1465 XL7 6NVI
-
-
SHOW
COVPDB1467 XL9 6NVK
-
-
SHOW