PDBsum entry 3vf9

Transferase/transferase inhibitor

PDB id: 3vf9

Contents

Protein chain

265 a.a.

Ligands

477

Waters ×43

PDB id:

3vf9

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of spleen tyrosine kinase syk catalytic domain with thienopyrazolylindole inhibitor 027

Structure:

Tyrosine-protein kinase syk. Chain: a. Fragment: unp residues 343-635. Synonym: spleen tyrosine kinase. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: syk. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9.

Resolution:

2.30Å R-factor: 0.255 R-free: 0.267

Authors:

L.R.Mclean,Y.Zhang

Key ref:

L.R.McLean et al. (2012). X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase. Bioorg Med Chem Lett, 22, 3296-3300. PubMed id: 22464456

Date:

09-Jan-12 Release date: 02-May-12

Protein chain

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

Seq: 635 a.a.

Struc: 265 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 22:3296-3300 (2012)

PubMed id: 22464456

X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.

L.R.McLean, Y.Zhang, N.Zaidi, X.Bi, R.Wang, R.Dharanipragada, J.G.Jurcak, T.A.Gillespy, Z.Zhao, K.Y.Musick, Y.M.Choi, M.Barrague, J.Peppard, M.Smicker, M.Duguid, A.Parkar, J.Fordham, D.Kominos.

ABSTRACT

No abstract given.