PDBsum entry 3u6i

Transferase/transferase inhibitor

PDB id: 3u6i

Contents

Protein chain

281 a.a.

Ligands

044

Waters ×342

PDB id:

3u6i

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of c-met in complex with pyrazolone inhibitor 58a

Structure:

Hepatocyte growth factor receptor. Chain: a. Fragment: unp residues 1048-1315. Synonym: hgf receptor, hgf/sf receptor, proto-oncogenE C-met, scatter factor receptor, sf receptor, tyrosine-protein kinase met. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: met. Expressed in: trichoplusia ni. Expression_system_taxid: 7111.

Resolution:

2.10Å R-factor: 0.208 R-free: 0.257

Authors:

S.F.Bellon,D.A.Whittington,A.L.Long

Key ref:

M.H.Norman et al. (2012). Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives. J Med Chem, 55, 1858-1867. PubMed id: 22320343

Date:

12-Oct-11 Release date: 22-Feb-12

Protein chain

P08581  (MET_HUMAN) -  Hepatocyte growth factor receptor from Homo sapiens

Seq: 1390 a.a.

Struc: 281 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

J Med Chem 55:1858-1867 (2012)

PubMed id: 22320343

Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.

M.H.Norman, L.Liu, M.Lee, N.Xi, I.Fellows, N.D.D'Angelo, C.Dominguez, K.Rex, S.F.Bellon, T.S.Kim, I.Dussault.

ABSTRACT

No abstract given.