PDBsum entry 4xcu

Transferase/transferase inhibitor

PDB id: 4xcu

Contents

Protein chain

288 a.a.

Ligands

SO4

40M

Waters ×172

PDB id:

4xcu

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of fgfr4 with an irreversible inhibitor

Structure:

Fibroblast growth factor receptor 4. Chain: a. Fragment: unp residues 449-751. Synonym: fgfr-4. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: fgfr4, jtk2, tkf. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108

Resolution:

1.71Å R-factor: 0.196 R-free: 0.243

Authors:

J.L.Kim,C.Miduturu,B.Hodous,N.Brooijmans,N.Bifulco,T.Guzi

Key ref:

M.Hagel et al. (2015). First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov, 5, 424-437. PubMed id: 25776529 DOI: 10.1158/2159-8290.CD-14-1029

Date:

18-Dec-14 Release date: 01-Apr-15

Protein chain

P22455  (FGFR4_HUMAN) -  Fibroblast growth factor receptor 4 from Homo sapiens

Seq: 802 a.a.

Struc: 288 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

DOI no: 10.1158/2159-8290.CD-14-1029

Cancer Discov 5:424-437 (2015)

PubMed id: 25776529

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.

M.Hagel, C.Miduturu, M.Sheets, N.Rubin, W.Weng, N.Stransky, N.Bifulco, J.L.Kim, B.Hodous, N.Brooijmans, A.Shutes, C.Winter, C.Lengauer, N.E.Kohl, T.Guzi.

ABSTRACT

No abstract given.