1STC

CAMP-DEPENDENT PROTEIN KINASE, ALPHA-CATALYTIC SUBUNIT IN COMPLEX WITH STAUROSPORINE

1STC の概要

• エントリーDOI: 10.2210/pdb1stc/pdb
• 分子名称: CAMP-DEPENDENT PROTEIN KINASE, PROTEIN KINASE INHIBITOR, STAUROSPORINE, ... (4 entities in total)
• 機能のキーワード: protein kinase, staurosporine, camp, phosphorylation, complex (transferase-inhibitor), serine/threonine-protein kinase, complex (transferase-inhibitor) complex, complex (transferase/inhibitor)
• 由来する生物種: Bos taurus (cattle)
• 細胞内の位置: Cytoplasm: P00517
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 43479.34

構造登録者

Prade, L.,Engh, R.A.,Girod, A.,Kinzel, V.,Huber, R.,Bossemeyer, D. (登録日: 1997-10-10, 公開日: 1998-02-25, 最終更新日: 2024-11-20)

主引用文献

Prade, L.,Engh, R.A.,Girod, A.,Kinzel, V.,Huber, R.,Bossemeyer, D.
Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential.
Structure, 5:1627-1637, 1997

PubMed Abstract: Staurosporine inhibits most protein kinases at low nanomolar concentrations. As most tyrosine kinases, along with many serine/threonine kinases, are either proto oncoproteins or are involved in oncogenic signaling, the development of protein kinase inhibitors is a primary goal of cancer research. Staurosporine and many of its derivatives have significant biological effects, and are being tested as anticancer drugs. To understand in atomic detail the mode of inhibition and the parameters of high-affinity binding of staurosporine to protein kinases, the molecule was cocrystallized with the catalytic subunit of cAMP-dependent protein kinase.

PubMed: 9438863
DOI: 10.1016/S0969-2126(97)00310-9

実験手法

X-RAY DIFFRACTION (2.3 Å)