Structure of PDB 4rwj Chain A

Receptor sequence
>4rwjA (length=307) Species: 9606 (Homo sapiens) [Search protein sequence]
MAGVSEYELPEDPRWELPRDRLVLGKPLGEGAFGQVVLAEAIGLDKDKPN
RVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGP
LYVIVEYASKGNLREYLQARRPPGLEYSYNPSHNPEEQLSSKDLVSCAYQ
VARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKK
TNGRLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVE
ELFKLLKEGHRMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRI
VALTSNQ
3D structure
PDB4rwj Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles' Heel of Targeted Therapy.
ChainA
Resolution2.489 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D623 A625 R627 N628 D641
Catalytic site (residue number reindexed from 1) D167 A169 R171 N172 D185
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine kinase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 66T A L484 G485 F489 A512 K514 E531 M535 I545 V561 A564 S565 G567 L630 D641 L28 G29 F33 A56 K58 E75 M79 I89 V105 A108 S109 G111 L174 D185 MOAD: Kd=2nM
PDBbind-CN: -logKd/Ki=8.70,Kd=2nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005007 fibroblast growth factor receptor activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:4rwj, PDBe:4rwj, PDBj:4rwj
PDBsum4rwj
PubMed25686244
UniProtP11362|FGFR1_HUMAN Fibroblast growth factor receptor 1 (Gene Name=FGFR1)

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