PDBsum entry 3qqu

Transferase/transferase inhibitor

PDB id: 3qqu

Contents

Protein chains

285 a.a.

Ligands

01P ×4

Waters ×163

PDB id:

3qqu

Name:

Transferase/transferase inhibitor

Title:

Cocrystal structure of unphosphorylated igf with pyrimidine 8

Structure:

Insulin-like growth factor 1 receptor. Chain: a, b, c, d. Fragment: unp residues 988-1286. Synonym: insulin-like growth factor i receptor, igf-i receptor. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: igf1r. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108.

Resolution:

2.90Å R-factor: 0.273 R-free: 0.302

Authors:

X.Huang

Key ref:

J.L.Buchanan et al. (2011). Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. Bioorg Med Chem Lett, 21, 2394-2399. PubMed id: 21414779

Date:

16-Feb-11 Release date: 20-Apr-11

Protein chains

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

Seq: 1367 a.a.

Struc: 285 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 21:2394-2399 (2011)

PubMed id: 21414779

Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.

J.L.Buchanan, J.R.Newcomb, D.P.Carney, S.C.Chaffee, L.Chai, R.Cupples, L.F.Epstein, P.Gallant, Y.Gu, J.C.Harmange, K.Hodge, B.E.Houk, X.Huang, J.Jona, S.Joseph, H.T.Jun, R.Kumar, C.Li, J.Lu, T.Menges, M.J.Morrison, P.M.Novak, S.van der Plas, R.Radinsky, P.E.Rose, S.Sawant, J.R.Sun, S.Surapaneni, S.M.Turci, K.Xu, E.Yanez, H.Zhao, X.Zhu.

ABSTRACT

No abstract given.