Structure of PDB 3qqu Chain D

Receptor sequence

>3qquD (length=292) Species: 9606 (Homo sapiens)

PDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEA
ASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLK
SYLRSLRPEMLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMV
AEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYS
DVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFE
LMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN

3D structure

• PDB: 3qqu Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
• Chain: D
• Resolution: 2.9 Å

Enzymatic activity

• Catalytic site (original residue number in PDB): D1132 R1136 N1137 D1150 E1159
• Catalytic site (residue number reindexed from 1): D142 R146 N147 D160 E169
• 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	01P	D	L1002 G1003 Q1004 V1010 A1028 E1077 M1079 G1082 M1139 D1150 M1153	L17 G18 Q19 V25 A43 E92 M94 G97 M149 D160 M163	BindingDB: IC50=2.4nM

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

Cellular Component

• GO:0016020 membrane

External links

• PDB: RCSB:3qqu, PDBe:3qqu, PDBj:3qqu
• PDBsum: 3qqu
• PubMed: 21414779
• UniProt: P08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)