PDBsum entry 2xa4

Transferase

PDB id: 2xa4

Contents

Protein chain

278 a.a. *

Ligands

AZ5 ×2

Waters ×308

* Residue conservation analysis

PDB id:

2xa4

Name:

Transferase

Title:

Inhibitors of jak2 kinase domain

Structure:

Tyrosine-protein kinase jak2. Chain: a, b. Fragment: kinase domain residues 835-1132. Synonym: janus kinase 2, jak-2. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli bl21(de3). Expression_system_taxid: 469008. Expression_system_variant: star.

Resolution:

2.04Å R-factor: 0.200 R-free: 0.245

Authors:

J.Read,I.Green,H.Pollard,T.Howard,R.Mott

Key ref:

S.Ioannidis et al. (2011). Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. J Med Chem, 54, 262-276. PubMed id: 21138246

Date:

26-Mar-10 Release date: 15-Dec-10

Protein chains

O60674  (JAK2_HUMAN) -  Tyrosine-protein kinase JAK2 from Homo sapiens

Seq: 1132 a.a.

Struc: 278 a.a.*

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

Enzyme reactions

• Enzyme class: E.C.2.7.10.2 - non-specific 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 54:262-276 (2011)

PubMed id: 21138246

Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.

S.Ioannidis, M.L.Lamb, T.Wang, L.Almeida, M.H.Block, A.M.Davies, B.Peng, M.Su, H.J.Zhang, E.Hoffmann, C.Rivard, I.Green, T.Howard, H.Pollard, J.Read, M.Alimzhanov, G.Bebernitz, K.Bell, M.Ye, D.Huszar, M.Zinda.

ABSTRACT

No abstract given.