Discovery of an oral potent selective inhibitor of hematopoietic prostaglandin D synthase (HPGDS)

Chris P. Carron, John I. Trujillo, Kirk L. Olson, Wei Huang, Bruce C. Hamper, Tom Dice, Bradley E. Neal, Matthew J. Pelc, Jacqueline E. Day, Douglas C. Rohrer, James R. Kiefer, Joseph B. Moon, Barbara A. Schweitzer, Tanisha D. Blake, Steve R. Turner, Rhonda Woerndle, Brenda L. Case, Christine P. Bono, Vickie M. Dilworth, Christie L. Funckes-ShippyBecky L. Hood, Gina M. Jerome, Christine M. Kornmeier, Melissa R. Radabaugh, Melanie L. Williams, Michael S. Davies, Craig D. Wegner, Dean J. Welsch, William M. Abraham, Chad J. Warren, Martin E. Dowty, Fengmei Hua, Anup Zutshi, Jerry Z. Yang, Atli Thorarensen

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

Abstract

Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH 2 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.

Original languageEnglish (US)
Pages (from-to)59-63
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume1
Issue number2
DOIs
StatePublished - May 13 2010

Keywords

  • airway allergy, inflammatory processes, cyclooxygenase (COX)
  • Hematopoietic prostaglandin D synthase (HPGDS)
  • PGH, PGD

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

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