Literature DB >> 19250823

Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.

Kimberly O Cameron1, Bruce A Lefker, Hua Z Ke, Mei Li, Michael P Zawistoski, Christina M Tjoa, Ann S Wright, Shari L DeNinno, Vishwas M Paralkar, Thomas A Owen, Li Yu, David D Thompson.   

Abstract

Sulfonamides, exemplified by 3a, were identified as highly selective EP(2) agonists. Lead optimization led to the identification of CP-533536, 7f, a potent and selective EP(2) agonist. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

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Year:  2009        PMID： 19250823     DOI： 10.1016/j.bmcl.2009.01.059

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

2.  Influence of Pain and Analgesia on Orthopedic and Wound-healing Models in Rats and Mice.

Authors:  Monika K Huss; Stephen A Felt; Cholawat Pacharinsak
Journal:  Comp Med       Date:  2019-09-27       Impact factor: 0.982

3.  Discovery of G Protein-Biased EP2 Receptor Agonists.

Authors:  Seiji Ogawa; Toshihide Watanabe; Isamu Sugimoto; Kazumi Moriyuki; Yoshikazu Goto; Shinsaku Yamane; Akio Watanabe; Kazuma Tsuboi; Atsushi Kinoshita; Hideo Kigoshi; Kousuke Tani; Toru Maruyama
Journal:  ACS Med Chem Lett       Date:  2016-01-04       Impact factor: 4.345

Review 4.  Prostaglandin receptor EP2 in the crosshairs of anti-inflammation, anti-cancer, and neuroprotection.

Authors:  Jianxiong Jiang; Ray Dingledine
Journal:  Trends Pharmacol Sci       Date:  2013-06-21       Impact factor: 14.819

Review 5.  Prostanoid receptor EP2 as a therapeutic target.

Authors:  Thota Ganesh
Journal:  J Med Chem       Date:  2013-12-04       Impact factor: 7.446

6.  Prostaglandin E2 signals through PTGER2 to regulate sclerostin expression.

Authors:  Damian C Genetos; Clare E Yellowley; Gabriela G Loots
Journal:  PLoS One       Date:  2011-03-16       Impact factor: 3.240

7.  In Vitro and In Vivo Validation of EP2-Receptor Agonism to Selectively Achieve Inhibition of Mast Cell Activity.

Authors:  Judith Plaza; Rosa Torres; Adrián Urbano; César Picado; Fernando de Mora
Journal:  Allergy Asthma Immunol Res       Date:  2020-07       Impact factor: 5.764

Review 8.  EP2 Antagonists (2011-2021): A Decade's Journey from Discovery to Therapeutics.

Authors:  Madison N Sluter; Ruida Hou; Lexiao Li; Nelufar Yasmen; Ying Yu; Jiawang Liu; Jianxiong Jiang
Journal:  J Med Chem       Date:  2021-08-05       Impact factor: 8.039

9.  Novel high-throughput myofibroblast assays identify agonists with therapeutic potential in pulmonary fibrosis that act via EP2 and EP4 receptors.

Authors:  Patrick Sieber; Anny Schäfer; Raphael Lieberherr; François Le Goff; Manuel Stritt; Richard W D Welford; John Gatfield; Oliver Peter; Oliver Nayler; Urs Lüthi
Journal:  PLoS One       Date:  2018-11-28       Impact factor: 3.240
  9 in total

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