6WEW

Crystal structures of human E-NPP 1: bound to N-{4-[(7-methoxyquinolin-4-yl)oxy]phenyl}sulfuric diamide

これはPDB形式変換不可エントリーです。

6WEW の概要

• エントリーDOI: 10.2210/pdb6wew/pdb
• 分子名称: Ectonucleotide pyrophosphatase/phosphodiesterase family member 1, 1,2-ETHANEDIOL, beta-D-mannopyranose-(1-3)-beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... (11 entities in total)
• 機能のキーワード: human e-npp 1; drug discovery; inhibitors, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• 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: 215035.33

構造登録者

Peat, T.S.,Dennis, M.,Newman, J. (登録日: 2020-04-03, 公開日: 2020-09-09, 最終更新日: 2023-10-18)

主引用文献

Dennis, M.L.,Newman, J.,Dolezal, O.,Hattarki, M.,Surjadi, R.N.,Nuttall, S.D.,Pham, T.,Nebl, T.,Camerino, M.,Khoo, P.S.,Monahan, B.J.,Peat, T.S.
Crystal structures of human ENPP1 in apo and bound forms.
Acta Crystallogr D Struct Biol, 76:889-898, 2020

PubMed Abstract: Cancer is one of the leading causes of mortality in humans, and recent work has focused on the area of immuno-oncology, in which the immune system is used to specifically target cancerous cells. Ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) is an emerging therapeutic target in human cancers owing to its role in degrading cyclic GMP-AMP (cGAMP), an agonist of the stimulator of interferon genes (STING). The available structures of ENPP1 are of the mouse enzyme, and no structures are available with anything other than native nucleotides. Here, the first X-ray crystal structures of the human ENPP1 enzyme in an apo form, with bound nucleotides and with two known inhibitors are presented. The availability of these structures and a robust crystallization system will allow the development of structure-based drug-design campaigns against this attractive cancer therapeutic target.

PubMed: 32876064
DOI: 10.1107/S2059798320010505

実験手法

X-RAY DIFFRACTION (2.73 Å)