1QZ6

Structure of rabbit actin in complex with jaspisamide A

1QZ6 の概要

• エントリーDOI: 10.2210/pdb1qz6/pdb
• 関連するPDBエントリー: 1QZ5
• 関連するBIRD辞書のPRD_ID: PRD_900003
• 分子名称: Actin, alpha skeletal muscle, beta-D-fructofuranose-(2-1)-alpha-D-glucopyranose, ADENOSINE-5'-TRIPHOSPHATE, ... (6 entities in total)
• 機能のキーワード: actin, trisoxazole, toxin, jaspisamide a, structural protein
• 由来する生物種: Oryctolagus cuniculus (rabbit)
• 細胞内の位置: Cytoplasm, cytoskeleton: P68135
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 43622.19

構造登録者

Klenchin, V.A.,Allingham, J.S.,King, R.,Tanaka, J.,Marriott, G.,Rayment, I. (登録日: 2003-09-15, 公開日: 2003-11-11, 最終更新日: 2020-07-29)

主引用文献

Klenchin, V.A.,Allingham, J.S.,King, R.,Tanaka, J.,Marriott, G.,Rayment, I.
Trisoxazole macrolide toxins mimic the binding of actin-capping proteins to actin
Nat.Struct.Biol., 10:1058-1063, 2003

PubMed Abstract: Marine macrolide toxins of trisoxazole family target actin with high affinity and specificity and have promising pharmacological properties. We present X-ray structures of actin in complex with two members of this family, kabiramide C and jaspisamide A, at a resolution of 1.45 and 1.6 A, respectively. The structures reveal the absolute stereochemistry of these toxins and demonstrate that their trisoxazole ring interacts with actin subdomain 1 while the aliphatic side chain is inserted into the hydrophobic cavity between actin subdomains 1 and 3. The binding site is essentially the same as the one occupied by the actin-capping domain of the gelsolin superfamily of proteins. The structural evidence suggests that actin filament severing and capping by these toxins is also analogous to that of gelsolin. Consequently, these macrolides may be viewed as small molecule biomimetics of an entire class of actin-binding proteins.

PubMed: 14578936
DOI: 10.1038/nsb1006

実験手法

X-RAY DIFFRACTION (1.6 Å)