Structure of PDB 2wkm Chain A

Receptor sequence
>2wkmA (length=286) Species: 9606 (Homo sapiens) [Search protein sequence]
NPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKKIHCA
VKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLP
YMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAAR
NCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQ
KFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYC
PDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTF
3D structure
PDB2wkm Structure Based Drug Design of Crizotinib (Pf-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (C-met) Kinase and Anaplastic Lymphoma Kinase (Alk).
ChainA
Resolution2.2 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1204 A1206 R1208 N1209 D1222 A1243
Catalytic site (residue number reindexed from 1) D146 A148 R150 N151 D164 A185
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 PFY A V1092 L1140 P1158 Y1159 M1160 H1162 G1163 M1211 A1221 D1222 A1226 Y1230 S1342 F1344 V34 L82 P100 Y101 M102 H104 G105 M153 A163 D164 A168 Y172 S284 F286 MOAD: ic50=9nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase 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:2wkm, PDBe:2wkm, PDBj:2wkm
PDBsum2wkm
PubMed21812414
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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