PDBsum entry 4mkc

Transferase/transferase inhibitor

PDB id: 4mkc

Contents

Protein chain

303 a.a.

Ligands

GOL ×2

4MK

Waters ×175

PDB id:

4mkc

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of anaplastic lymphoma kinase complexed with ldk378

Structure:

Alk tyrosine kinase receptor. Chain: a. Fragment: catalytic domain residues 1072-1410. Synonym: anaplastic lymphoma kinase. Engineered: yes. Mutation: yes

Source:

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

Resolution:

2.01Å R-factor: 0.173 R-free: 0.218

Authors:

C.C.Lee,G.Spraggon

Key ref:

L.Friboulet et al. (2014). The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer. Cancer Discov, 4, 662-673. PubMed id: 24675041 DOI: 10.1158/2159-8290.CD-13-0846

Date:

04-Sep-13 Release date: 09-Apr-14

Protein chain

Q9UM73  (ALK_HUMAN) -  ALK tyrosine kinase receptor from Homo sapiens

Seq: 1620 a.a.

Struc: 303 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-13-0846

Cancer Discov 4:662-673 (2014)

PubMed id: 24675041

The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer.

L.Friboulet, N.Li, R.Katayama, C.C.Lee, J.F.Gainor, A.S.Crystal, P.Y.Michellys, M.M.Awad, N.Yanagitani, S.Kim, A.C.Pferdekamper, J.Li, S.Kasibhatla, F.Sun, X.Sun, S.Hua, P.McNamara, S.Mahmood, E.L.Lockerman, N.Fujita, M.Nishio, J.L.Harris, A.T.Shaw, J.A.Engelman.

ABSTRACT

No abstract given.