PDBsum entry 3qti

Transferase/transferase inhibitor

PDB id: 3qti

Contents

Protein chains

292 a.a.

Ligands

3QT ×2

GOL

Metals

_CL ×2

Waters ×395

PDB id:

3qti

Name:

Transferase/transferase inhibitor

Title:

C-met kinase in complex with nvp-bvu972

Structure:

Hepatocyte growth factor receptor. Chain: a, b. Fragment: kinase domain, residues 1050-1360. 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: spodoptera frugiperda. Expression_system_taxid: 7118

Resolution:

2.00Å R-factor: 0.184 R-free: 0.214

Authors:

B.A.Appleton

Key ref:

R.Tiedt et al. (2011). A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients. Cancer Res, 71, 5255-5264. PubMed id: 21697284 DOI: 10.1158/0008-5472.CAN-10-4433

Date:

22-Feb-11 Release date: 06-Jul-11

Protein chains

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

Seq: 1390 a.a.

Struc: 292 a.a.*

* PDB and UniProt seqs differ at 2 residue positions (black crosses)

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

DOI no: 10.1158/0008-5472.CAN-10-4433

Cancer Res 71:5255-5264 (2011)

PubMed id: 21697284

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.

R.Tiedt, E.Degenkolbe, P.Furet, B.A.Appleton, S.Wagner, J.Schoepfer, E.Buck, D.A.Ruddy, J.E.Monahan, M.D.Jones, J.Blank, D.Haasen, P.Drueckes, M.Wartmann, C.McCarthy, W.R.Sellers, F.Hofmann.

ABSTRACT

No abstract given.