2DQ7

Crystal Structure of Fyn kinase domain complexed with staurosporine

2DQ7 の概要

• エントリーDOI: 10.2210/pdb2dq7/pdb
• 分子名称: Proto-oncogene tyrosine-protein kinase Fyn, STAUROSPORINE (3 entities in total)
• 機能のキーワード: src family, kinase domain, staurosporine, transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: P06241
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 33111.91

構造登録者

Kinoshita, T.,Tada, T. (登録日: 2006-05-23, 公開日: 2006-07-04, 最終更新日: 2024-10-09)

主引用文献

Kinoshita, T.,Matsubara, M.,Ishiguro, H.,Okita, K.,Tada, T.
Structure of human Fyn kinase domain complexed with staurosporine.
Biochem.Biophys.Res.Commun., 346:840-844, 2006

PubMed Abstract: The tyrosine kinase Fyn is a member of the Src kinase family. Besides the role of Fyn in T cell signal transduction in concert with Lck, its excess activity in the brain is involved with conditions such as Alzheimer's and Parkinson's diseases. Therefore, inhibition of Fyn kinase may help counteract these nervous system disorders. Here, we solved the crystal structure of the human Fyn kinase domain complexed with staurosporine, a potent kinase inhibitor, at 2.8 A resolution. Staurosporine binds to the ATP-binding site of Fyn in a similar manner as in the Lck- and Csk-complexes. The small structural differences in the staurosporine-binding and/or -unbinding region among the three kinase domains may help obtaining the selective inhibitors against the respective kinases.

PubMed: 16782058
DOI: 10.1016/j.bbrc.2006.05.212

実験手法

X-RAY DIFFRACTION (2.8 Å)