3SMM

Crystal structure of human 14-3-3 sigma C38N/N166H in complex with task-3 peptide and stabilizer Fusicoccin J aglycone

3SMM の概要

• エントリーDOI: 10.2210/pdb3smm/pdb
• 関連するPDBエントリー: 2O98 3LW1 3MHR
• 分子名称: 14-3-3 protein sigma, TASK-3 peptide, Fusicoccin J aglycone, ... (6 entities in total)
• 機能のキーワード: helical protein, phosphoprotein, adapter protein, peptide binding protein, nucleus
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Cytoplasm: P31947
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 27893.73

構造登録者

Anders, C.,Schumacher, B.,Ottmann, C. (登録日: 2011-06-28, 公開日: 2012-07-11, 最終更新日: 2024-10-30)

主引用文献

Anders, C.,Higuchi, Y.,Koschinsky, K.,Bartel, M.,Schumacher, B.,Thiel, P.,Nitta, H.,Preisig-Muller, R.,Schlichthorl, G.,Renigunta, V.,Ohkanda, J.,Daut, J.,Kato, N.,Ottmann, C.
A semisynthetic fusicoccane stabilizes a protein-protein interaction and enhances the expression of K+ channels at the cell surface.
Chem. Biol., 20:583-593, 2013

PubMed Abstract: Small-molecule stabilization of protein-protein interactions is an emerging field in chemical biology. We show how fusicoccanes, originally identified as fungal toxins acting on plants, promote the interaction of 14-3-3 proteins with the human potassium channel TASK-3 and present a semisynthetic fusicoccane derivative (FC-THF) that targets the 14-3-3 recognition motif (mode 3) in TASK-3. In the presence of FC-THF, the binding of 14-3-3 proteins to TASK-3 was increased 19-fold and protein crystallography provided the atomic details of the effects of FC-THF on this interaction. We also tested the functional effects of FC-THF on TASK channels heterologously expressed in Xenopus oocytes. Incubation with 10 μM FC-THF was found to promote the transport of TASK channels to the cell membrane, leading to a significantly higher density of channels at the surface membrane and increased potassium current.

PubMed: 23601647
DOI: 10.1016/j.chembiol.2013.03.015

実験手法

X-RAY DIFFRACTION (2 Å)