1. Academic Validation
  2. 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)

  • ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z.
Chris P Carron 1 John I Trujillo 1 Kirk L Olson 1 Wei Huang 1 Bruce C Hamper 1 Tom Dice 1 Bradley E Neal 1 Matthew J Pelc 1 Jacqueline E Day 1 Douglas C Rohrer 1 James R Kiefer 1 Joseph B Moon 1 Barbara A Schweitzer 1 Tanisha D Blake 1 Steve R Turner 1 Rhonda Woerndle 1 Brenda L Case 1 Christine P Bono 1 Vickie M Dilworth 1 Christie L Funckes-Shippy 1 Becky L Hood 1 Gina M Jerome 1 Christine M Kornmeier 1 Melissa R Radabaugh 1 Melanie L Williams 1 Michael S Davies 1 Craig D Wegner 1 Dean J Welsch 1 William M Abraham 2 Chad J Warren 1 Martin E Dowty 1 Fengmei Hua 1 Anup Zutshi 1 Jerry Z Yang 1 Atli Thorarensen 1
Affiliations

Affiliations

  • 1 Pfizer Global Research and Development, 700 Chesterfield Parkway West, Chesterfield, Missouri 63017.
  • 2 Department of Research, Mount Sinai Medical Center, 4300 Alton Road, Miami Beach, Florida 33140.
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.

Keywords

Hematopoietic prostaglandin D synthase (HPGDS); PGD2; PGH2; airway allergy; inflammatory processes, cyclooxygenase (COX).

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