Structure of PDB 4u0i Chain A

Receptor sequence
>4u0iA (length=297) Species: 9606 (Homo sapiens) [Search protein sequence]
GNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIAA
MTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTL
VITEYCCYGDLLNFLRRKRDSFICSLALDLEDLLSFSYQVAKGMAFLASK
NCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWM
APESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEG
FRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTN
3D structure
PDB4u0i Ponatinib Inhibits Polyclonal Drug-Resistant KIT Oncoproteins and Shows Therapeutic Potential in Heavily Pretreated Gastrointestinal Stromal Tumor (GIST) Patients.
ChainA
Resolution2.0 Å
3D
structure
Catalytic site residues are labeled in the structure
[Spin on]
[Spin off]
[Reset orientation]

[High quality]
[Low quality]

[White background]
[Black background]

[Download]
[Download structure with residue number starting from 1]
Enzymatic activity
Catalytic site (original residue number in PDB) D792 R796 N797 D810
Catalytic site (residue number reindexed from 1) D156 R160 N161 D174
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 0LI A L595 A621 V622 K623 E640 T670 Y672 C673 I789 H790 R791 L799 C809 D810 F811 L31 A54 V55 K56 E73 T103 Y105 C106 I153 H154 R155 L163 C173 D174 F175 MOAD: ic50<11nM
PDBbind-CN: -logKd/Ki=8.22,IC50=6nM
BindingDB: IC50=1.7nM
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:4u0i, PDBe:4u0i, PDBj:4u0i
PDBsum4u0i
PubMed25239608
UniProtP10721|KIT_HUMAN Mast/stem cell growth factor receptor Kit (Gene Name=KIT)

[Back to BioLiP]