5VX1

Bak L100A

5VX1 の概要

• エントリーDOI: 10.2210/pdb5vx1/pdb
• 関連するPDBエントリー: 5VWV 5VWW 5VWX 5VWY 5VWZ 5VX0 5VX2 5VX3
• 分子名称: Bcl-2 homologous antagonist/killer (2 entities in total)
• 機能のキーワード: apoptosis, bcl-2 family, mutant
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 37990.48

構造登録者

Brouwer, J.M.,Colman, P.M.,Czabotar, P.E. (登録日: 2017-05-23, 公開日: 2017-11-15, 最終更新日: 2024-03-13)

主引用文献

Brouwer, J.M.,Lan, P.,Cowan, A.D.,Bernardini, J.P.,Birkinshaw, R.W.,van Delft, M.F.,Sleebs, B.E.,Robin, A.Y.,Wardak, A.,Tan, I.K.,Reljic, B.,Lee, E.F.,Fairlie, W.D.,Call, M.J.,Smith, B.J.,Dewson, G.,Lessene, G.,Colman, P.M.,Czabotar, P.E.
Conversion of Bim-BH3 from Activator to Inhibitor of Bak through Structure-Based Design.
Mol. Cell, 68:659-672.e9, 2017

PubMed Abstract: Certain BH3-only proteins transiently bind and activate Bak and Bax, initiating their oligomerization and the permeabilization of the mitochondrial outer membrane, a pivotal step in the mitochondrial pathway to apoptosis. Here we describe the first crystal structures of an activator BH3 peptide bound to Bak and illustrate their use in the design of BH3 derivatives capable of inhibiting human Bak on mitochondria. These BH3 derivatives compete for the activation site at the canonical groove, are the first engineered inhibitors of Bak activation, and support the role of key conformational transitions associated with Bak activation.

PubMed: 29149594
DOI: 10.1016/j.molcel.2017.11.001

実験手法

X-RAY DIFFRACTION (1.224 Å)