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Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)

  作者 CARRON CHRIS P; TRUJILLO JOHN I; OLSON KIRK L; HUANG WEI; HAMPER BRUCE C; DICE TOM; NEAL BRADLEY E; PELC MATTHEW J; DAY JACQUELINE E; ROHRER DOUGLAS C; KIEFER JAMES R; MOON JOSEPH B; SCHWEITZER BARBARA A; BLAKE TANISHA D; TURNER STEVE R; WOERNDLE RHONDA; CASE BRENDA L; BONO CHRISTINE P; DILWORTH VICKIE M; FUNCKESSHIPPY CHRISTIE L; HOOD BECKY L; JEROME GINA M; KORNMEIER CHRISTINE M; RADABAUGH MELISSA R; WILLIAMS MELANIE L; DAVIES MICHAEL S; WEGNER CRAIG D; WELSCH DEAN J; ABRAHAM WILLIAM M; WARREN CHAD J; DOWTY MARTIN E; HUA FENGMEI; ZUTSHI ANUP; YANG JERRY Z; THORARENSEN ATLI  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2010年1-2;  页码  59-63  
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[摘要]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.

 
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