PDBsum entry 5tr6

Transferase/transferase inhibitor

PDB id: 5tr6

Contents

Protein chain

272 a.a.

Ligands

7KG

EDO

Waters ×132

PDB id:

5tr6

Name:

Transferase/transferase inhibitor

Title:

Discovery of tak-659, an orally available investigational inhibitor of spleen tyrosine kinase (syk)

Structure:

Tyrosine-protein kinase syk. Chain: a. Fragment: unp residues 356-635. Synonym: spleen tyrosine kinase,p72-syk. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: syk. Expressed in: baculovirus expression vector pfastbac1-hm. Expression_system_taxid: 274590.

Resolution:

1.93Å R-factor: 0.195 R-free: 0.217

Authors:

J.Yano,A.Jennings,B.Lam,I.D.Hoffman

Key ref:

B.Lam et al. (2016). Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett, 26, 5947-5950. PubMed id: 27839918 DOI: 10.1016/j.bmcl.2016.10.087

Date:

25-Oct-16 Release date: 30-Nov-16

Protein chain

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

Seq: 635 a.a.

Struc: 272 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

DOI no: 10.1016/j.bmcl.2016.10.087

Bioorg Med Chem Lett 26:5947-5950 (2016)

PubMed id: 27839918

Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).

B.Lam, Y.Arikawa, J.Cramlett, Q.Dong, R.de Jong, V.Feher, C.E.Grimshaw, P.J.Farrell, I.D.Hoffman, A.Jennings, B.Jones, J.Matuszkiewicz, J.Miura, H.Miyake, S.R.Natala, L.Shi, M.Takahashi, E.Taylor, C.Wyrick, J.Yano, J.Zalevsky, Z.Nie.

ABSTRACT

No abstract given.