Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)
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DOI：
10.1021/ml900025z
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发表时间：
2010-05-01
影响因子：
4.2
通讯作者：
Thorarensen, Atli
中科院分区：
文献类型：
--
作者：
Carron, Chris P.;Trujillo, John I.;Thorarensen, Atli
造血前列腺素D合成酶（HPGDS）主要表达于肥大细胞、抗原呈递细胞和Th-2细胞中。HPGDS将PGH（2）转化为PGD（2），PGD（2）是一种被认为在气道过敏和炎症过程中起关键作用的介质。在这封信中，我们报告了一种口服有效的选择性HPGDS抑制剂的发现，该抑制剂可降低过敏性绵羊的抗原诱导反应。
Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH(2) into PGD(2), a mediator thought to play a pivotal role in airway allergy and inflammatory processes. In this letter, we report the discovery of an orally potent and selective inhibitor of HPGDS that reduces the antigen-induced response in allergic sheep.