Structure of PDB 6gqk Chain A

Receptor sequence

>6gqkA (length=305) Species: 9606 (Homo sapiens)

NYSYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAQGLIKSDA
AMTVAVKMLKPSAHSTEREALMSELKVLSYLGNHENIVNLLGACTHGGPT
LVITEYCCYGDLLNFLRRKRDEFVPYKVAPEDLYKDFLTLEHLLSFSYQV
AKGMAFLASKNCIHRDLAARNILLTHGNITKICDFGLARDIKNDSNYVDK
GNARLPVKWMAPESIFNSVYTFESDVWSYGIFLWELFSLGSSPYPGMPVD
SKFYKMIKEGFRMSSPEYAPAEMYDIMKTCWDADPDKRPTFKQIVQDIEK
QISES

3D structure

• PDB: 6gqk Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
• Chain: A
• Resolution: 2.31 Å

Enzymatic activity

• Catalytic site (original residue number in PDB): D792 R796 N797 D810
• Catalytic site (residue number reindexed from 1): D166 R170 N171 D184
• 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	F88	A	L595 V603 A621 I653 Y672 C673 G676 L799 C809 D810 F811	L29 V37 A55 I87 Y106 C107 G110 L173 C183 D184 F185

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

External links

• PDB: RCSB:6gqk, PDBe:6gqk, PDBj:6gqk
• PDBsum: 6gqk
• PubMed: 30204441
• UniProt: P10721|KIT_HUMAN Mast/stem cell growth factor receptor Kit (Gene Name=KIT)