3CF6

Structure of Epac2 in complex with cyclic-AMP and Rap

3CF6 の概要

• エントリーDOI: 10.2210/pdb3cf6/pdb
• 関連するPDBエントリー: 2BYV
• 分子名称: Rap guanine nucleotide exchange factor (GEF) 4, Ras-related protein Rap-1b, 6-(6-AMINO-PURIN-9-YL)-2-THIOXO-TETRAHYDRO-2-FURO[3,2-D][1,3,2]DIOXAPHOSPHININE-2,7-DIOL, ... (5 entities in total)
• 機能のキーワード: epac, rapgef4, rap, rap1b, camp, sp-camps, gef, gunanine nucleotide exchange factor, g-protein, gtp-binding, nucleotide-binding, signaling protein regulator-gtp-binding protein complex, signaling protein-gtp-binding protein complex, signaling protein/gtp-binding protein
• 由来する生物種: Mus musculus (mouse); 詳細
• 細胞内の位置: Cell membrane: P61224
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 99084.95

構造登録者

Rehmann, H.,Arias-Palomo, E.,Hadders, M.A.,Schwede, F.,Llorca, O.,Bos, J.L. (登録日: 2008-03-02, 公開日: 2008-07-29, 最終更新日: 2023-11-01)

主引用文献

Rehmann, H.,Arias-Palomo, E.,Hadders, M.A.,Schwede, F.,Llorca, O.,Bos, J.L.
Structure of Epac2 in complex with a cyclic AMP analogue and RAP1B
Nature, 455:124-127, 2008

PubMed Abstract: Epac proteins are activated by binding of the second messenger cAMP and then act as guanine nucleotide exchange factors for Rap proteins. The Epac proteins are involved in the regulation of cell adhesion and insulin secretion. Here we have determined the structure of Epac2 in complex with a cAMP analogue (Sp-cAMPS) and RAP1B by X-ray crystallography and single particle electron microscopy. The structure represents the cAMP activated state of the Epac2 protein with the RAP1B protein trapped in the course of the exchange reaction. Comparison with the inactive conformation reveals that cAMP binding causes conformational changes that allow the cyclic nucleotide binding domain to swing from a position blocking the Rap binding site towards a docking site at the Ras exchange motif domain.

PubMed: 18660803
DOI: 10.1038/nature07187

実験手法

X-RAY DIFFRACTION (2.2 Å)