PDBsum entry 4f65

Transferase/transferase inhibitor

PDB id: 4f65

Contents

Protein chains

279 a.a.

Ligands

SO4 ×4

EDO ×10

0S9 ×2

Waters ×190

PDB id:

4f65

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with compound 8

Structure:

Fibroblast growth factor receptor 1. Chain: a, b. Fragment: kinase domain (unp residues 458-765). Synonym: fgfr-1, basic fibroblast growth factor receptor 1, bfgfr, bfgf-r-1, fms-like tyrosine kinase 2, flt-2, n-sam, proto-oncogenE C- fgr. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: fgfr1, bfgfr, cek, fgfbr, flg, flt2, hbgfr. Expressed in: escherichia coli. Expression_system_taxid: 562

Resolution:

2.26Å R-factor: 0.204 R-free: 0.236

Authors:

R.A.Norman,J.Breed,D.Ogg

Key ref:

R.A.Norman et al. (2012). Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase. J Med Chem, 55, 5003-5012. PubMed id: 22612866

Date:

14-May-12 Release date: 06-Jun-12

Protein chains

P11362  (FGFR1_HUMAN) -  Fibroblast growth factor receptor 1 from Homo sapiens

Seq: 822 a.a.

Struc: 279 a.a.*

* PDB and UniProt seqs differ at 1 residue position (black cross)

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

J Med Chem 55:5003-5012 (2012)

PubMed id: 22612866

Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.

R.A.Norman, A.K.Schott, D.M.Andrews, J.Breed, K.M.Foote, A.P.Garner, D.Ogg, J.P.Orme, J.H.Pink, K.Roberts, D.A.Rudge, A.P.Thomas, A.G.Leach.

ABSTRACT

No abstract given.