Literature DB >> 20471829

Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.

John Colucci1, Michael Boyd, Carl Berthelette, Jean-Francois Chiasson, Zhaoyin Wang, Yves Ducharme, Rick Friesen, Mark Wrona, Jean-Francois Levesque, Danielle Denis, Marie-Claude Mathieu, Rino Stocco, Alex G Therien, Patsy Clarke, Steve Rowland, Daigen Xu, Yongxin Han.   

Abstract

The discovery of a highly potent and selective EP(4) antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model. Copyright 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20471829     DOI： 10.1016/j.bmcl.2010.04.065

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


  6 in total

1.  AKAP-dependent sensitization of Ca(v) 3.2 channels via the EP(4) receptor/cAMP pathway mediates PGE(2) -induced mechanical hyperalgesia.

Authors:  Fumiko Sekiguchi; Yuka Aoki; Maiko Nakagawa; Daiki Kanaoka; Yuta Nishimoto; Maho Tsubota-Matsunami; Rumi Yamanaka; Shigeru Yoshida; Atsufumi Kawabata
Journal:  Br J Pharmacol       Date:  2013-02       Impact factor: 8.739

2.  Evaluation of a candidate anti-arthritic drug using the mouse collagen antibody induced arthritis model and clinically relevant biomarkers.

Authors:  Andrew T Bender; Mark Spyvee; Takashi Satoh; Benjamin Gershman; Tyler Teceno; Laurette Burgess; Vipul Kumar; Yin Wu; Hua Yang; Yueyun Ding; Sandeep Akare; Qian Chen
Journal:  Am J Transl Res       Date:  2013-01-21       Impact factor: 4.060

3.  Combination of EP4 antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both lymphocytes and myeloid cells.

Authors:  Yun Wang; Long Cui; Peter Georgiev; Latika Singh; Yanyan Zheng; Ying Yu; Jeff Grein; Chunsheng Zhang; Eric S Muise; David L Sloman; Heidi Ferguson; Hongshi Yu; Cristina St Pierre; Pranal J Dakle; Vincenzo Pucci; James Baker; Andrey Loboda; Doug Linn; Christopher Brynczka; Doug Wilson; Brian B Haines; Brian Long; Richard Wnek; Svetlana Sadekova; Michael Rosenzweig; Andrew Haidle; Yongxin Han; Sheila H Ranganath
Journal:  Oncoimmunology       Date:  2021-03-18       Impact factor: 8.110

4.  External oxidant-compatible phosphorus(III)-directed site-selective C-H carbonylation.

Authors:  Ben Dong; Jiasheng Qian; Mingjie Li; Zheng-Jun Wang; Minyan Wang; Dingyi Wang; Chengkai Yuan; Ying Han; Yue Zhao; Zhuangzhi Shi
Journal:  Sci Adv       Date:  2020-12-16       Impact factor: 14.136

Review 5.  E-type prostanoid receptor 4 (EP4) in disease and therapy.

Authors:  Viktoria Konya; Gunther Marsche; Rufina Schuligoi; Akos Heinemann
Journal:  Pharmacol Ther       Date:  2013-03-21       Impact factor: 12.310

6.  TRPV1 Channel Activated by the PGE2/EP4 Pathway Mediates Spinal Hypersensitivity in a Mouse Model of Vertebral Endplate Degeneration.

Authors:  Sijing Liu; Qiong Wang; Ziyi Li; Lei Ma; Ting Li; Yukun Li; Na Wang; Chang Liu; Peng Xue; Chuan Wang
Journal:  Oxid Med Cell Longev       Date:  2021-08-21       Impact factor: 6.543
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.