High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors
High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors
复制标题
DOI：
10.1107/s1744309110020828
复制
发表时间：
2010-06-01
影响因子：
0.9
通讯作者：
Urade, Yoshihiro
中科院分区：
文献类型：
--
作者：
Takahashi, Sachiko;Tsurumura, Toshiharu;Urade, Yoshihiro
人造血前列腺素D合酶（H-PGDS; EC 5.3.99.2）在肥大细胞和Th 2细胞中产生前列腺素D-2，一种过敏和炎症介质。H-PGDS已与新型抑制剂一起结晶，其半最大抑制浓度（IC 50）在低纳摩尔范围内，通过国际空间站上俄罗斯服务舱上的反扩散方法进行。使用SPring-8同步加速器辐射，在100 K下，与IC 50值为50 nM的抑制剂复合的H-PGDS的微重力生长晶体的X射线衍射扩展到1.1埃分辨率，这是迄今为止该蛋白质获得的最高分辨率之一。
Human haematopoietic prostaglandin D synthase (H-PGDS; EC 5.3.99.2) produces prostaglandin D-2, an allergic and inflammatory mediator, in mast cells and Th2 cells. H-PGDS has been crystallized with novel inhibitors with half-maximal inhibitory concentrations (IC50) in the low nanomolar range by the counter-diffusion method onboard the Russian Service Module on the International Space Station. The X-ray diffraction of a microgravity-grown crystal of H-PGDS complexed with an inhibitor with an IC50 value of 50 nM extended to 1.1 angstrom resolution at 100 K using SPring-8 synchrotron radiation, which is one of the highest resolutions obtained to date for this protein.