PDBsum entry 3a4o

Transferase

PDB id: 3a4o

Contents

Protein chain

259 a.a. *

Ligands

STU

* Residue conservation analysis

PDB id:

3a4o

Name:

Transferase

Title:

Lyn kinase domain

Structure:

Tyrosine-protein kinase lyn. Chain: x. Fragment: residues in unp 233-512. Engineered: yes

Source:

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

Resolution:

3.00Å R-factor: 0.293 R-free: 0.324

Authors:

N.Miyano,T.Kinoshita,T.Tada

Key ref:

N.Miyano et al. (2009). Structural basis for the inhibitor recognition of human Lyn kinase domain. Bioorg Med Chem Lett, 19, 6557-6560. PubMed id: 19857964

Date:

11-Jul-09 Release date: 08-Dec-09

Protein chain

P07948  (LYN_HUMAN) -  Tyrosine-protein kinase Lyn from Homo sapiens

Seq: 512 a.a.

Struc: 259 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 19:6557-6560 (2009)

PubMed id: 19857964

Structural basis for the inhibitor recognition of human Lyn kinase domain.

N.Miyano, T.Kinoshita, R.Nakai, Y.Kirii, K.Yokota, T.Tada.

ABSTRACT

Human Lyn tyrosine kinase is expressed in hematopoietic tissues and plays crucial roles in the signal transduction of hematopoietic immune system. Its excess activity is involved in several tumors. The crystal structure has revealed that the potent inhibitor staurosporine binds to human Lyn kinase domain at the ATP-binding site. The remarkable structural features of the staurosporine-binding region will offer valuable structural insights for the structure-based design of novel Lyn-selective inhibitors.