PDBsum entry 4hge

Transferase/transferase inhibitor

PDB id: 4hge

Contents

Protein chain

286 a.a.

Ligands

15V ×2

Waters ×182

PDB id:

4hge

Name:

Transferase/transferase inhibitor

Title:

Jak2 kinase (jh1 domain) in complex with compound 8

Structure:

Tyrosine-protein kinase jak2. Chain: a, b. Fragment: jh1 domain, unp residues 833-1132. Synonym: janus kinase 2, jak-2. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: jak2. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108

Resolution:

2.30Å R-factor: 0.182 R-free: 0.227

Authors:

C.Eigenbrot,M.Ultsch

Key ref:

E.J.Hanan et al. (2012). Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. J Med Chem, 55, 10090-10107. PubMed id: 23061660

Date:

08-Oct-12 Release date: 24-Oct-12

Protein chains

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

Seq: 1132 a.a.

Struc: 286 a.a.

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 55:10090-10107 (2012)

PubMed id: 23061660

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

E.J.Hanan, A.van Abbema, K.Barrett, W.S.Blair, J.Blaney, C.Chang, C.Eigenbrot, S.Flynn, P.Gibbons, C.A.Hurley, J.R.Kenny, J.Kulagowski, L.Lee, S.R.Magnuson, C.Morris, J.Murray, R.M.Pastor, T.Rawson, M.Siu, M.Ultsch, A.Zhou, D.Sampath, J.P.Lyssikatos.

ABSTRACT

No abstract given.