摘要:
A method of designing an anti-allergic agent, sleep controlling agent, anti-obestic agent and remedy for brain injury acting via the inhibition of biosynthesis of prostaglandin D2. Crystal of a complex of human origin hematopoietic prostaglandin D synthase, glutathione, and a substrate analog or an inhibitor, etc are prepared and the three-dimensional structural coordinate of each atom in the complex is determined by X-ray crystal analysis.
摘要:
It is intended to provide a method of designing an antiallergic agent, a sleep controlling agent, an antiobestic and a remedy for brain injury acting via the inhibition of the biosynthesis of prostaglandin D2. Crystals of a complex of human-origin hematopoietic prostaglandin D synthase, glutathione and a substrate analog or an inhibitor, etc. are prepared and the three-dimensional structural coordinate of each atom in the complex is determined by X-ray crystal analysis.
摘要:
An object of the present invention is to provide a method which is able to prevent or improve the progress of myolytic diseases such as muscular dystrophy. Such an object is able to be solved by a method where an effective dose of an inhibitor for hematopoietic prostaglandin D synthase (H-PGDS) or an antagonist to prostaglandin D receptor is administered to a patient who needs it. The present invention also provides a method for screening compounds which are able to prevent the progress of myolytic diseases and to improve it using human H-PGDS overexpressed transgenic mice.
摘要:
An object of the present invention is to provide a method which is able to prevent or improve the progress of myolytic diseases such as muscular dystrophy. Such an object is able to be solved by a method where an effective dose of an inhibitor for hematopoietic prostaglandin D synthase (H-PGDS) or an antagonist to prostaglandin D receptor is administered to a patient who needs it. The present invention also provides a method for screening compounds which are able to prevent the progress of myolytic diseases and to improve it using human H-PGDS overexpressed transgenic mice.
摘要:
A medicament having an inhibitory activity against hematopoietic prostaglandin D2 synthase, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein X represents a group represented by the formula —N═C(R5)— or the formula —NH—CH(R5)—, R1, R2, R3, and R4 represent a hydrogen atom, a halogen atom, a C1 to C6 alkyl group, or a hydroxy group, R5 represents a C1 to C6 alkyl group or a C6 to C10 aryl group, and R represents an amino group.
摘要:
The present application provides a human gene over-expressing animal, which is a non-human animal carrying a human hematopoietic prostaglandin D2 synthase gene in its somatic cell chromosome and expressing a large amount of human prostaglandin D2 synthase, wherein the animal is one obtained through ontogenesis of a totipotency cell of a non-human animal or offspring of the obtained animal, and the totipotency cell is introduced with said synthase gene. The present application also provides a method of using the transgenic animal for testing in vivo activity of a candidate for anti-allergy medicines, sleep-controlling substances and candidates for anti-obesity.
摘要翻译:本申请提供了一种人基因过表达动物,其是在其体细胞染色体中携带人造血前列腺素D 2 N 2合酶基因的非人动物,并表达大量人前列腺素D 其中所述动物是通过非人动物全能细胞或所获得的动物的后代的发生获得的动物,并且所述合成细胞与所述合酶基因一起引入。 本申请还提供了使用转基因动物测试抗过敏药物候选物,睡眠控制物质和抗肥胖候选物的体内活性的方法。
摘要:
There are provided a compound for treatment or prevention of brain injury caused by diseases such as cerebrovascular disorder, brain degenerative disease and demyelinating disease and a method for screening the same. Brain injury in which prostaglandin D2 is participated is treated or prevented by inhibition of hematopoietic prostaglandin D synthase induced in microglia cell or macrophage of brain injury area by diseases such as cerebrovascular disorder, brain degenerative disease or demyelinating disease or by inhibition of activation of prostaglandin D receptor expressed in astroglia cell around the injured area. There is also provided a method of testing those pharmaceutical substances using a transgenic mouse in which human hematopoietic prostaglandin D synthase is expressed in large amounts.
摘要:
Muscle degenerative diseases can be detected in the early stage and the therapeutic efficacy of a therapeutic agent and/or a therapy method for the diseases can be determined by measuring 11,15-dioxo-9α-hydroxy-2,3,4,5-tetranorprostan-1,20-dioic acid (referred to as “Tetranor-PGDM”, hereinbelow) in a sample isolated from a subject.
摘要:
The present invention provides a benzimidazole compound represented by Formula (I) wherein X1 is oxygen or carbonyl, and R1 is a furan ring having 1 to 3 substituents or a pyrrole ring that may have 1 to 3 substituents; excluding compounds represented by Formula (I) wherein at least one of the substituents is a phosphoric acid group or a phosphoric ester group; or a salt thereof. The benzimidazole compound or salt thereof has excellent prostaglandin synthase inhibitory activity, and is useful as an agent for preventing and/or treating diseases in which prostaglandin D2 or metabolites thereof participates, such as allergic and inflammatory diseases, and as inhibitor for the exacerbation of Alzheimer's disease or cerebral damage.
摘要:
Provided are: a method for predicting the onset of pregnancy-induced hypertension (PIH) by precisely detecting abnormalities that occur before the onset of PIH (where such abnormalities have been impossible to detect by various conventional testing methods for PIH) while imposing less of a burden on a subject; a method for evaluating a fetus and placental functions in PIH; and a method for detecting PIH, which comprises measuring the level of human lipocalin-type prostaglandin D synthase (L-PGDS) in a body fluid sample collected from a subject.