PDBsum entry 5t68

Transferase/transferase inhibitor

PDB id: 5t68

Contents

Protein chains

266 a.a.

Ligands

77V ×2

Waters ×23

PDB id:

5t68

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of syk catalytic domain in complex with a furo[3,2- d]pyrimidine

Structure:

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

Source:

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

Resolution:

2.93Å R-factor: 0.188 R-free: 0.281

Authors:

M.A.Argiriadi,M.Hoemann,N.Wilson,D.Banach,A.Burchat,D.Calderwood, B.Clapham,P.Cox,D.B.Duignan,D.Konopacki,G.Somal,A.Vasudevan

Key ref:

M.Hoemann et al. (2016). Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. Bioorg Med Chem Lett, 26, 5562-5567. PubMed id: 27789138 DOI: 10.1016/j.bmcl.2016.09.077

Date:

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

Protein chains

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

Seq: 635 a.a.

Struc: 266 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.2016.09.077

Bioorg Med Chem Lett 26:5562-5567 (2016)

PubMed id: 27789138

Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.

M.Hoemann, N.Wilson, M.Argiriadi, D.Banach, A.Burchat, D.Calderwood, B.Clapham, P.Cox, D.B.Duignan, D.Konopacki, G.Somal, A.Vasudevan.

ABSTRACT

No abstract given.