Literature DB >> 24900177

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

Chris P Carron1, John I Trujillo1, Kirk L Olson1, Wei Huang1, Bruce C Hamper1, Tom Dice1, Bradley E Neal1, Matthew J Pelc1, Jacqueline E Day1, Douglas C Rohrer1, James R Kiefer1, Joseph B Moon1, Barbara A Schweitzer1, Tanisha D Blake1, Steve R Turner1, Rhonda Woerndle1, Brenda L Case1, Christine P Bono1, Vickie M Dilworth1, Christie L Funckes-Shippy1, Becky L Hood1, Gina M Jerome1, Christine M Kornmeier1, Melissa R Radabaugh1, Melanie L Williams1, Michael S Davies1, Craig D Wegner1, Dean J Welsch1, William M Abraham2, Chad J Warren1, Martin E Dowty1, Fengmei Hua1, Anup Zutshi1, Jerry Z Yang1, Atli Thorarensen1.   

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.

Entities:  

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

Year:  2010        PMID： 24900177      PMCID： PMC4007851          DOI： 10.1021/ml900025z

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  21 in total

1.  Cloning and crystal structure of hematopoietic prostaglandin D synthase.

Authors:  Y Kanaoka; H Ago; E Inagaki; T Nanayama; M Miyano; R Kikuno; Y Fujii; N Eguchi; H Toh; Y Urade; O Hayaishi
Journal:  Cell       Date:  1997-09-19       Impact factor: 41.582

Review 2.  Lipocalin-type and hematopoietic prostaglandin D synthases as a novel example of functional convergence.

Authors:  Yoshihiro Urade; Naomi Eguchi
Journal:  Prostaglandins Other Lipid Mediat       Date:  2002-08       Impact factor: 3.072

3.  Prostaglandin D2 as a mediator of allergic asthma.

Authors:  T Matsuoka; M Hirata; H Tanaka; Y Takahashi; T Murata; K Kabashima; Y Sugimoto; T Kobayashi; F Ushikubi; Y Aze; N Eguchi; Y Urade; N Yoshida; K Kimura; A Mizoguchi; Y Honda; H Nagai; S Narumiya
Journal:  Science       Date:  2000-03-17       Impact factor: 47.728

4.  Mammalian class Sigma glutathione S-transferases: catalytic properties and tissue-specific expression of human and rat GSH-dependent prostaglandin D2 synthases.

Authors:  I R Jowsey; A M Thomson; J U Flanagan; P R Murdock; G B Moore; D J Meyer; G J Murphy; S A Smith; J D Hayes
Journal:  Biochem J       Date:  2001-11-01       Impact factor: 3.857

Review 5.  The allergic cascade: review of the most important molecules in the asthmatic lung.

Authors:  Karolien Bloemen; Sandra Verstraelen; Rosette Van Den Heuvel; Hilda Witters; Inge Nelissen; Greet Schoeters
Journal:  Immunol Lett       Date:  2007-08-15       Impact factor: 3.685

6.  Novel prostaglandin D synthase inhibitors generated by fragment-based drug design.

Authors:  Morten Hohwy; Loredana Spadola; Britta Lundquist; Paul Hawtin; Jan Dahmén; Ib Groth-Clausen; Ewa Nilsson; Sofia Persdotter; Karin von Wachenfeldt; Rutger H A Folmer; Karl Edman
Journal:  J Med Chem       Date:  2008-03-15       Impact factor: 7.446

7.  The bronchoconstrictor effect of inhaled prostaglandin D2 in normal and asthmatic men.

Authors:  C C Hardy; C Robinson; A E Tattersfield; S T Holgate
Journal:  N Engl J Med       Date:  1984-07-26       Impact factor: 91.245

8.  Essential role for hematopoietic prostaglandin D2 synthase in the control of delayed type hypersensitivity.

Authors:  Seema G Trivedi; Justine Newson; Ravindra Rajakariar; Thomas S Jacques; Robert Hannon; Yoshihide Kanaoka; Naomi Eguchi; Paul Colville-Nash; Derek W Gilroy
Journal:  Proc Natl Acad Sci U S A       Date:  2006-03-17       Impact factor: 11.205

Review 9.  Antagonism of the prostaglandin D2 receptors DP1 and CRTH2 as an approach to treat allergic diseases.

Authors:  Roy Pettipher; Trevor T Hansel; Richard Armer
Journal:  Nat Rev Drug Discov       Date:  2007-04       Impact factor: 84.694

10.  Expression of prostaglandin D synthase and the prostaglandin D2 receptors DP and CRTH2 in human nasal mucosa.

Authors:  François Nantel; Carolyn Fong; Sonia Lamontagne; D Hamish Wright; Adel Giaid; Martin Desrosiers; Kathleen M Metters; Gary P O'Neill; François G Gervais
Journal:  Prostaglandins Other Lipid Mediat       Date:  2004-01       Impact factor: 3.072
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  4 in total

1.  Structure-metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines.

Authors:  Sabin Llona-Minguez; Artin Ghassemian; Pawel Baranczewski; Matthieu Desroses; Tobias Koolmeister; Per Artursson; Martin Scobie; Thomas Helleday
Journal:  Medchemcomm       Date:  2017-07-04       Impact factor: 3.597

Review 2.  Prostaglandins and Their Receptors in Eosinophil Function and As Therapeutic Targets.

Authors:  Miriam Peinhaupt; Eva M Sturm; Akos Heinemann
Journal:  Front Med (Lausanne)       Date:  2017-07-19

3.  Obesity-induced changes in lipid mediators persist after weight loss.

Authors:  A Hernandez-Carretero; N Weber; M R La Frano; W Ying; J Lantero Rodriguez; D D Sears; V Wallenius; E Börgeson; J W Newman; O Osborn
Journal:  Int J Obes (Lond)       Date:  2017-11-01       Impact factor: 5.095

4.  Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon.

Authors:  Yu-Meng Miao; Ya-Jing Zhang; Si-Miao Qiao; Yu-Feng Xia; Zhi-Feng Wei; Yue Dai
Journal:  Acta Pharmacol Sin       Date:  2020-07-21       Impact factor: 6.150
  4 in total

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