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PDBsum entry 5tq5
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protein ligands links
Transferase/transferase inhibitor PDB id
5tq5

 

 

 

 

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JSmol PyMol  
Contents
Protein chain
291 a.a.
Ligands
7GX
Waters ×34
PDB id:
5tq5
Name: Transferase/transferase inhibitor
Title: Design and synthesis of a pan-jak kinase inhibitor clinical candidate (pf-06263276) suitable for inhaled and topical delivery for the treatment of inflammatory diseases of the lungs and skin
Structure: Tyrosine-protein kinase jak2. Chain: a. Fragment: unp residues 837-1132. Synonym: janus kinase 2,jak-2. Engineered: yes. Mutation: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: jak2. Expressed in: homo sapiens. Expression_system_taxid: 9606
Resolution:
2.30Å     R-factor:   0.282     R-free:   0.332
Authors: J.Chrencik,P.Jones
Key ref: P.Jones et al. (2017). Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin. J Med Chem, 60, 767-786. PubMed id: 27983835 DOI: 10.1021/acs.jmedchem.6b01634
Date:
23-Oct-16     Release date:   11-Jan-17    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
O60674  (JAK2_HUMAN) -  Tyrosine-protein kinase JAK2 from Homo sapiens
Seq:
Struc: 		 
Seq:
Struc: 		 
Seq:
Struc: 		1132 a.a.
291 a.a.*
Key:    PfamA domain  Secondary structure
* 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.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H+
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: 10.1021/acs.jmedchem.6b01634 J Med Chem 60:767-786 (2017)
PubMed id: 27983835  
 
 
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
P.Jones, R.I.Storer, Y.A.Sabnis, F.M.Wakenhut, G.A.Whitlock, K.S.England, T.Mukaiyama, C.M.Dehnhardt, J.W.Coe, S.W.Kortum, J.E.Chrencik, D.G.Brown, R.M.Jones, J.R.Murphy, T.Yeoh, P.Morgan, I.Kilty.
 
  ABSTRACT  
 
No abstract given.

 

 

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