Structure of PDB 3lco Chain A

Receptor sequence
>3lcoA (length=293) Species: 9606 (Homo sapiens) [Search protein sequence]
KIIEFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKED
AVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGP
VLVITEYCCYGDLLNFLRRKAEAMLGPSGRPLELRDLLHFSSQVAQGMAF
LASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVRLPVKWM
APESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDG
YQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQ
3D structure
PDB3lco Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
ChainA
Resolution3.4 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D778 R782 N783 D796
Catalytic site (residue number reindexed from 1) D160 R164 N165 D178
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 LC0 A L588 A614 K616 V647 E664 C666 L785 G795 D796 F797 L30 A56 K58 V89 E106 C108 L167 G177 D178 F179 PDBbind-CN: -logKd/Ki=6.84,IC50=143nM
BindingDB: IC50=143nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0004714 transmembrane receptor protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:3lco, PDBe:3lco, PDBj:3lco
PDBsum3lco
PubMed20137931
UniProtP07333|CSF1R_HUMAN Macrophage colony-stimulating factor 1 receptor (Gene Name=CSF1R)

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