High-quality crystals of human haematopoietic prostaglandin D synthase with novel inhibitors.
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.
Takahashi
Sachiko
S
Confocal Science Inc., Japan. takahashis@confsci.co.jp
Tsurumura
Toshiharu
T
Aritake
Kosuke
K
Furubayashi
Naoki
N
Sato
Masaru
M
Yamanaka
Mari
M
Hirota
Erika
E
Sano
Satoshi
S
Kobayashi
Tomoyuki
T
Tanaka
Tetsuo
T
Inaka
Koji
K
Tanaka
Hiroaki
H
Urade
Yoshihiro
Y
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*
D004791:Enzyme Inhibitors; D054834:Lipocalins; D019746:Intramolecular Oxidoreductases; C022466:prostaglandin R2 D-isomerase