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

ABSTRACT: Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH2 into PGD2, 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.

SUBMITTER: Carron CP

PROVIDER: S-EPMC4007851 | biostudies-literature | 2010 May

REPOSITORIES: biostudies-literature

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

Carron Chris P CP Trujillo John I JI Olson Kirk L KL Huang Wei W Hamper Bruce C BC Dice Tom T Neal Bradley E BE Pelc Matthew J MJ Day Jacqueline E JE Rohrer Douglas C DC Kiefer James R JR Moon Joseph B JB Schweitzer Barbara A BA Blake Tanisha D TD Turner Steve R SR Woerndle Rhonda R Case Brenda L BL Bono Christine P CP Dilworth Vickie M VM Funckes-Shippy Christie L CL Hood Becky L BL Jerome Gina M GM Kornmeier Christine M CM Radabaugh Melissa R MR Williams Melanie L ML Davies Michael S MS Wegner Craig D CD Welsch Dean J DJ Abraham William M WM Warren Chad J CJ Dowty Martin E ME Hua Fengmei F Zutshi Anup A Yang Jerry Z JZ Thorarensen Atli A

ACS medicinal chemistry letters 20100202 2

Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH2 into PGD2, 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. ...[more]

PMID: 24900177

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