title: High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors.
abstract: 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 (IC(50)) 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 IC(50) value of 50 nM extended to 1.1 A resolution at 100 K using SPring-8 synchrotron radiation, which is one of the highest resolutions obtained to date for this protein.
authors.affiliation: Confocal Science Inc., Japan. takahashis@confsci.co.jp
authors.forename: Sachiko
authors.initials: S
authors.lastname: Takahashi
authors.forename: Toshiharu
authors.initials: T
authors.lastname: Tsurumura
authors.forename: Kosuke
authors.initials: K
authors.lastname: Aritake
authors.forename: Naoki
authors.initials: N
authors.lastname: Furubayashi
authors.forename: Masaru
authors.initials: M
authors.lastname: Sato
authors.forename: Mari
authors.initials: M
authors.lastname: Yamanaka
authors.forename: Erika
authors.initials: E
authors.lastname: Hirota
authors.forename: Satoshi
authors.initials: S
authors.lastname: Sano
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Kobayashi
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Tanaka
authors.forename: Koji
authors.initials: K
authors.lastname: Inaka
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Tanaka
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Urade
mesh_terms: D003460:Crystallization; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry*; D006801:Humans; D019746:Intramolecular Oxidoreductases / Q000037:antagonists & inhibitors / Q000737:chemistry*; D054834:Lipocalins / Q000037:antagonists & inhibitors / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D054834:Lipocalins; D019746:Intramolecular Oxidoreductases; C022466:prostaglandin R2 D-isomerase