PDBsum entry 3srv

Transferase/transferase inhibitor

PDB id: 3srv

Contents

Protein chains

263 a.a.

Ligands

S19 ×2

GOL ×4

Waters ×472

PDB id:

3srv

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of spleen tyrosine kinase (syk) in complex with a diaminopyrimidine carboxamide inhibitor

Structure:

Tyrosine-protein kinase syk. Chain: a. Fragment: kinase domain (unp residues 360-635). Synonym: spleen tyrosine kinase. Engineered: yes. Tyrosine-protein kinase syk. Chain: b. Fragment: kinase domain (unp residues 360-635). Synonym: spleen tyrosine kinase.

Source:

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

Resolution:

1.95Å R-factor: 0.188 R-free: 0.241

Authors:

D.O.Somers,M.Neu

Key ref:

J.Liddle et al. (2011). Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg Med Chem Lett, 21, 6188-6194. PubMed id: 21903390

Date:

07-Jul-11 Release date: 21-Sep-11

Protein chains

P43405  (KSYK_HUMAN) -  Tyrosine-protein kinase SYK from Homo sapiens

Seq: 635 a.a.

Struc: 263 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

Bioorg Med Chem Lett 21:6188-6194 (2011)

PubMed id: 21903390

Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.

J.Liddle, F.L.Atkinson, M.D.Barker, P.S.Carter, N.R.Curtis, R.P.Davis, C.Douault, M.C.Dickson, D.Elwes, N.S.Garton, M.Gray, T.G.Hayhow, C.I.Hobbs, E.Jones, S.Leach, K.Leavens, H.D.Lewis, S.McCleary, M.Neu, V.K.Patel, A.G.Preston, C.Ramirez-Molina, T.J.Shipley, P.A.Skone, N.Smithers, D.O.Somers, A.L.Walker, R.J.Watson, G.G.Weingarten.

ABSTRACT

No abstract given.