2VCG

Crystal structure of a HDAC-like protein HDAH from Bordetella sp. with the bound inhibitor ST-17

2VCG の概要

• エントリーDOI: 10.2210/pdb2vcg/pdb
• 関連するPDBエントリー: 1ZZ0 1ZZ1 1ZZ3
• 分子名称: HISTONE DEACETYLASE-LIKE AMIDOHYDROLASE, ZINC ION, POTASSIUM ION, ... (7 entities in total)
• 機能のキーワード: hdah, inhibitor, hdac-like amidohydrolase, hydrolase, histone deacetylase-like amidohydrolase
• 由来する生物種: ALCALIGENES SP.
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 163590.61

構造登録者

Dickmanns, A.,Strasser, A.,Ficner, R. (登録日: 2007-09-24, 公開日: 2008-01-08, 最終更新日: 2023-12-13)

主引用文献

Schaefer, S.,Saunders, L.,Eliseeva, E.,Velena, A.,Jung, M.,Schwienhorst, A.,Strasser, A.,Dickmanns, A.,Ficner, R.,Schlimme, S.,Sippl, W.,Verdin, E.,Jung, M.
Phenylalanine-Containing Hydroxamic Acids as Selective Inhibitors of Class Iib Histone Deacetylases (Hdacs).
Bioorg.Med.Chem., 16:2011-, 2008

PubMed Abstract: We synthesized biarylalanine-containing hydroxamic acids and tested them on immunoprecipitated HDAC1 and HDAC6 and show a subtype selectivity for HDAC6 that was confirmed in cells by Western blot (tubulin vs histones). We obtained an X-ray structure with a HDAC6-selective inhibitor with the bacterial deacetylase HDAH. Docking studies were carried out using HDAC1 and HDAC6 protein models. Antiproliferative activity was shown on cancer cells for selected compounds.

PubMed: 18054239
DOI: 10.1016/J.BMC.2007.10.092

実験手法

X-RAY DIFFRACTION (1.9 Å)