阻害剤開発のための2種のプロスタグランジン合成酵素の構造と機能

抄録

The structural based drug-design (SBDD) is one of the useful methods for producing a novel medicine. We recently succeeded in X-ray crystallographic determination of two target molecules. One is human hematopoietic prostaglandin (PG) D synthase (H-PGDS) that produces PGD₂ as an allergic mediator in mast cells and Th2 cells. The other is Trypanosoma brucei PGF_2α synthase (TbPGFS), a member of the aldo-ketoreductase superfamily, catalyzes the NADPH-dependent reduction of PGH₂ to PGF_2α, whose overproduction during trypanosomiasis causes miscarriage in infected female subjects. In this report, we introduce the recent progress in the research of the high resolution structures of human H-PGDS and TbPGFS useful for SBDD.