1. Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)
- Author
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Barbara A. Schweitzer, Atli Thorarensen, Michael S. Davies, Steve R. Turner, Matthew James Pelc, James R. Kiefer, Brenda L. Case, Christie L. Funckes-Shippy, Jacqueline E. Day, Fengmei Hua, Dice Tom, William M. Abraham, Bradley E. Neal, John I. Trujillo, Joseph B. Moon, Blake Tanisha Danielle Rowe, Wei Huang, Craig D. Wegner, Dean Welsch, Chris P. Carron, Anup Zutshi, Bruce C. Hamper, Chad J. Warren, Rhonda S. Woerndle, Christine M. Kornmeier, Vickie M. Dilworth, Melanie L. Williams, Martin E. Dowty, Olson Kirk Lang, Melissa R. Radabaugh, Becky L. Hood, Jerry Z. Yang, Douglas C. Rohrer, Gina M. Jerome, and Christine P. Bono
- Subjects
Allergy ,Mediator ,Hematopoietic prostaglandin D synthase ,business.industry ,Organic Chemistry ,Drug Discovery ,medicine ,lipids (amino acids, peptides, and proteins) ,Pharmacology ,medicine.disease ,business ,Biochemistry - 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.
- Published
- 2010