PDBsum entry 3o23

Transferase/transferase inhibitor

PDB id: 3o23

Contents

Protein chain

293 a.a.

Ligands

MQY

Waters ×85

PDB id:

3o23

Name:

Transferase/transferase inhibitor

Title:

Human unphosphorylated igf1-r kinase domain in complex with an hydantoin inhibitor

Structure:

Insulin-like growth factor 1 receptor. Chain: a. Fragment: kinase domain. Synonym: insulin-like growth factor i receptor, igf-i receptor, insulin-like growth factor 1 receptor alpha chain, insulin-like growth factor 1 receptor beta chain. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: igf1r. Expressed in: escherichia coli. Expression_system_taxid: 562

Resolution:

2.10Å R-factor: 0.238 R-free: 0.278

Authors:

S.Maignan,J.P.Guilloteau,A.Dupuy

Key ref:

D.Lesuisse et al. (2011). Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors. Bioorg Med Chem Lett, 21, 2224-2228. PubMed id: 21441024

Date:

22-Jul-10 Release date: 04-May-11

Protein chain

P08069  (IGF1R_HUMAN) -  Insulin-like growth factor 1 receptor from Homo sapiens

Seq: 1367 a.a.

Struc: 293 a.a.

Enzyme reactions

• Enzyme class: E.C.2.7.10.1 - receptor protein-tyrosine kinase.
• Reaction: L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H⁺

Molecule diagrams generated from .mol files obtained from the KEGG ftp site

Added reference

Bioorg Med Chem Lett 21:2224-2228 (2011)

PubMed id: 21441024

Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.

D.Lesuisse, J.Mauger, C.Nemecek, S.Maignan, J.Boiziau, G.Harlow, A.Hittinger, S.Ruf, H.Strobel, A.Nair, K.Ritter, J.L.Malleron, A.Dagallier, Y.El-Ahmad, J.P.Guilloteau, H.Guizani, H.Bouchard, C.Venot.

ABSTRACT

No abstract given.