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Literature summary for 5.3.99.2 extracted from

  • Inoue, T.; Okano, Y.; Kado, Y.; Aritake, K.; Irikura, D.; Uodome, N.; Okazaki, N.; Kinugasa, S.; Shishitani, H.; Matsumura, H.; Kai, Y.; Urade, Y.
    First determination of the inhibitor complex structure of human hematopoietic prostaglandin D synthase (2004), J. Biochem., 135, 279-283.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
crystals of H-PGDS are first grown by hanging-drop vapor diffusion method with PEG6000 as the precipitant at 20°C in the presence of 5 mM Mg2+ and the native crystals are then soaked in the precipitant solution with a saturating concentration of 2-(2'-benzothiazolyl)-5-styryl-3-(4'-phthalhydrazyl) tetrazolium chloride for 2 weeks. Structure of the enzyme complexed with 2-(2'-benzothiazolyl)-5-styryl-3-(4'-phthalhydrazyl) tetrazolium chloride at 1.9 A resolution in the presence of Mg2+. The styryl group of the inhibitor penetrates to the bottom of the active site cleft, and the tetrazole ring is stabilized by the stacking interaction with TRp104, inducing large movement around the alpha5-helix, which causes the space group of the complex crystal to change from P2(1) to P1 upon binding of 2-(2'-benzothiazolyl)-5-styryl-3-(4'-phthalhydrazyl) tetrazolium chloride Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(2'-benzothiazolyl)-5-styryl-3-(4'-phthalhydrazyl) tetrazolium chloride IC50: 0.0362 mM in presence of EDTA, 0.0981 in presence of Mg2+ Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
hematopoietic cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
H-PGDS
-
Homo sapiens
Hematopoietic prostaglandin D synthase
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
glutathione KM for glutathione is decreased from 0.0006 mM in presence of EDTA to 0.00014 mM in presence of Mg2+ Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0362
-
IC50: 0.0362 mM in presence of EDTA, 0.0981 in presence of Mg2+ Homo sapiens 2-(2'-benzothiazolyl)-5-styryl-3-(4'-phthalhydrazyl) tetrazolium chloride