Crystal structure determination of microsomal prostaglandin E2 synthase 1 with the open active site.

具有开放活性位点的微粒体前列腺素 E2 合酶 1 的晶体结构测定。

• 批准号: 23570153
• 负责人: AGO Hideo
• 金额: $ 3.41万
• 依托单位: The Institute of Physical and Chemical Research
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2011
• 资助国家: 日本
• 起止时间: 2011 至 2013
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-23570153/
• 关键词: 膜タンパク質; Ｘ線結晶構造解析; 結晶化; 界面活性剤; ロイコトリエン; X線結晶構造解析; 炎症; 脂質

Human membrane protein MPGES1, which is a responsible protein for biosynthesis of prostaglandin E2 as a proinflammatory lipid mediator, was crystallized in a lipidic meso crystallization method. MPGES1 in the lipidic meso phase could be a structure more similar to a structure in cell membrane due to the similarity between the structures of the lipidic meso phase and cell membrane. The inhibitors for MPGES1 were found out from the candidates from the in silico screening targeted to the active site of leukotriene C4 synthase belonging in the same protein family with MPGES1. These results will contribute the elucidation of the structure basis of molecular functions of MPGES1.

人膜蛋白MPGES1是前列腺素E_2作为促炎性脂质介质生物合成的关键蛋白，采用脂质介晶法进行结晶。由于脂类介相与细胞膜的结构相似，脂类介相的MPGES1可能是更类似于细胞膜的结构。通过对白三烯C4合成酶活性部位的电子筛选，发现了MPGES1的抑制物，与MPGES1属于同一蛋白家族。这些结果将有助于阐明MPGES1分子功能的结构基础。

项目成果

The catalytic architecture of leukotriene C4 synthase with two arginine residues.

具有两个精氨酸残基的白三烯 C4 合酶的催化结构。

• DOI: 10.1074/jbc.m110.150177
• 发表时间: 2011
• 期刊: The Journal of biological chemistry
• 作者: Saino,Hiromichi;Ukita,Yoko;Ago,Hideo;Irikura,Daisuke;Nisawa,Atsushi;Ueno,Go;Yamamoto,Masaki;Kanaoka,Yoshihide;Lam,BingK;Austen,KFrank;Miyano,Masashi
• 通讯作者: Miyano,Masashi

Seleno-detergent MAD phasing of leukotriene C4 synthase in complex with dodecyl-β-D-selenomaltoside.

白三烯 C4 合酶与十二烷基-β-D-硒麦芽糖苷复合物的硒去垢剂 MAD 定相。

• 发表时间: 2011
• 期刊: Acta Crystallogr Sect F Struct Biol Cryst Commun.
• 作者: Saino Hiromichi;Ago Hideo;Ukita Yoko;Miyano Masashi.
• 通讯作者: Miyano Masashi.

X-ray protein crystallography free from radiation damage at SACLA

SACLA 的 X 射线蛋白质晶体学无辐射损伤

• 发表时间: 2012
• 作者: Ago;H.
• 通讯作者: H.