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

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 po...

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Published in:ACS medicinal chemistry letters 2010-05, Vol.1 (2), p.59-63
Main Authors: 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, Funckes-Shippy, 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
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Language:English
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Letter
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Summary: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml900025z