PDBsum entry 5lwm

Transferase

PDB id: 5lwm

Contents

Protein chain

290 a.a.

Ligands

79T

PHU

EDO ×6

Waters ×213

PDB id:

5lwm

Name:

Transferase

Title:

Crystal structure of jak3 in complex with compound 4 (fm381)

Structure:

Tyrosine-protein kinase jak3. Chain: a. Synonym: janus kinase 3,jak-3,leukocyte janus kinase,l-jak. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: jak3. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108

Resolution:

1.55Å R-factor: 0.166 R-free: 0.204

Authors:

A.Chaikuad,M.Forster,S.Mukhopadhyay,K.Kupinska,K.Ellis,P.Mahajan, N.Burgess-Brown,A.M.Edwards,C.H.Arrowsmith,C.Bountra,S.A.Laufer, S.Knapp,Structural Genomics Consortium (Sgc)

Key ref:

M.Forster et al. (2016). Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. Cell Chem Biol, 23, 1335-1340. PubMed id: 27840070 DOI: 10.1016/j.chembiol.2016.10.008

Date:

18-Sep-16 Release date: 26-Oct-16

Protein chain

P52333  (JAK3_HUMAN) -  Tyrosine-protein kinase JAK3 from Homo sapiens

Seq: 1124 a.a.

Struc: 290 a.a.*

* PDB and UniProt seqs differ at 3 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

DOI no: 10.1016/j.chembiol.2016.10.008

Cell Chem Biol 23:1335-1340 (2016)

PubMed id: 27840070

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.

M.Forster, A.Chaikuad, S.M.Bauer, J.Holstein, M.B.Robers, C.R.Corona, M.Gehringer, E.Pfaffenrot, K.Ghoreschi, S.Knapp, S.A.Laufer.

ABSTRACT

No abstract given.