3RI1: Catalytic domain of FGFR2 kinase

Crystal structure of the catalytic domain of FGFR2 kinase in complex with ARQ 069. Determined by X-ray diffraction at 2.1 Å resolution. Released 4 May 2011.

Method
X-ray diffraction
Resolution
2.1 Å
Organism
Homo sapiens
Chains
2
Atoms
4,968
Mol. weight
72.94 kDa
Ligands
3RH
Released
4 May 2011

Explore 3RI1 in 3D Show helices and sheets RCSB PDB PDBe

Secondary structure: helices and β-sheets

3RI1 contains 33 α-helices and 28 β-strands across 2 chains. Residue ranges use author residue numbering, as in the PDB file, from PDBe. To see them in 3D, choose the Cartoon representation with Secondary structure coloring: helices, sheets and coils get different colors.

Chain A: 16 helices, 14 β-strands

ElementResiduesLengthSheet
β-strand47511
α-helix478-4803
β-strand481-48771
β-strand494-50181
β-strand511-51881
β-strand52412
α-helix525-54016
β-strand54713
β-strand550-55451
β-strand561-56551
β-strand57113
α-helix572-5787
α-helix597-5993
α-helix600-61920
β-strand622-62324
α-helix629-6313
β-strand632-63433
β-strand640-64233
β-strand649-65024
β-strand66615
α-helix667-6693
α-helix672-6765
α-helix682-69716
α-helix701-7022
α-helix709-7179
α-helix722-7254
α-helix730-73910
α-helix744-7463
α-helix748-7492
α-helix750-76415
Chain B: 17 helices, 14 β-strands
ElementResiduesLengthSheet
β-strand47516
α-helix478-4803
β-strand481-48776
β-strand494-50186
β-strand511-51886
β-strand52415
α-helix525-54016
β-strand54717
β-strand550-55456
β-strand561-56556
β-strand57117
α-helix572-5776
α-helix597-5993
α-helix600-61920
β-strand622-62328
α-helix629-6313
β-strand632-63437
β-strand640-64237
β-strand649-65028
β-strand66612
α-helix667-6693
α-helix672-6765
α-helix682-69716
α-helix701-7022
α-helix709-7113
α-helix712-7176
α-helix722-7254
α-helix730-73910
α-helix744-7463
α-helix748-7492
α-helix750-76516

Molecules and chains

MoleculeChainsTypeLengthOrganismUniProt
Fibroblast growth factor receptor 2A, Bprotein313Homo sapiensP21802 (AlphaFold model)
Sequence of entity 1 (A, B), FASTA
>3RI1_1 Fibroblast growth factor receptor 2 (chains A, B)
GSPMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVA
VKMLKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREY
LRARRPPGMEYSYDINRVPEEQMTFKDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVT
ENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWE
IFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVE
DLDRILTLTTNEE

Ligands and cofactors

IDNameFormulaCopies
3RH(6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amineC18 H15 N32

Water and common crystallization additives (SO4) are not listed.

Primary citation

A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor. Eathiraj, S., Palma, R., Hirschi, M. et al. J Biol Chem (2011) 286:20677-20687. DOI 10.1074/jbc.M110.213736 · PubMed

Other PDB entries of the same protein (UniProt P21802 (AlphaFold model), which also has an AlphaFold model), best resolution first:

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