PDBsum entry 5toz

Transferase/transferase inhibitor

PDB id: 5toz

Contents

Protein chain

278 a.a.

Ligands

7H4

SO4

Waters ×232

PDB id:

5toz

Name:

Transferase/transferase inhibitor

Title:

Jak3 with covalent inhibitor pf-06651600

Structure:

Tyrosine-protein kinase jak3. Chain: a. Fragment: unp residues 812-1124. 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:

1.98Å R-factor: 0.184 R-free: 0.216

Authors:

F.F.Vajdos

Key ref:

J.B.Telliez et al. (2016). Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. Acs Chem Biol, 11, 3442-3451. PubMed id: 27791347 DOI: 10.1021/acschembio.6b00677

Date:

19-Oct-16 Release date: 09-Nov-16

Protein chain

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

Seq: 1124 a.a.

Struc: 278 a.a.*

* PDB and UniProt seqs differ at 1 residue position (black cross)

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: 10.1021/acschembio.6b00677

Acs Chem Biol 11:3442-3451 (2016)

PubMed id: 27791347

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

J.B.Telliez, M.E.Dowty, L.Wang, J.Jussif, T.Lin, L.Li, E.Moy, P.Balbo, W.Li, Y.Zhao, K.Crouse, C.Dickinson, P.Symanowicz, M.Hegen, M.E.Banker, F.Vincent, R.Unwalla, S.Liang, A.M.Gilbert, M.F.Brown, M.Hayward, J.Montgomery, X.Yang, J.Bauman, J.I.Trujillo, A.Casimiro-Garcia, F.F.Vajdos, L.Leung, K.F.Geoghegan, A.Quazi, D.Xuan, L.Jones, E.Hett, K.Wright, J.D.Clark, A.Thorarensen.

ABSTRACT

No abstract given.