Literature DB >> 25408836

Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.

Satoshi Itadani1, Shinya Takahashi1, Masaki Ima1, Tetsuya Sekiguchi1, Manabu Fujita1, Yoshisuke Nakayama1, Jun Takeuchi1.   

Abstract

The benzoxazine derivative, (2S)-4-(3-carboxypropyl)-8-{[4-(4-phenylbutoxy)benzoyl]amino}-3,4-dihydro-2H-1,4-benzoxazine-2-carboxylic acid (19, ONO-2050297), was identified as the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.

Entities:  

Keywords:  CysLT1; CysLT2; Cysteinyl leukotrienes; asthma; dual antagonist

Year:  2014        PMID： 25408836      PMCID： PMC4233365          DOI： 10.1021/ml500298y

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


  23 in total

Review 1.  Cysteinyl leukotriene receptors.

Authors:  Jilly F Evans
Journal:  Prostaglandins Other Lipid Mediat       Date:  2002-08       Impact factor: 3.072

Review 2.  Treatment of asthma with antileukotrienes: first line or last resort therapy?

Authors:  Sven-Erik Dahlén
Journal:  Eur J Pharmacol       Date:  2006-02-28       Impact factor: 4.432

3.  Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.

Authors:  Xiaowu Dong; Yanmei Zhao; Xueqin Huang; Kana Lin; Jianzhong Chen; Erqing Wei; Tao Liu; Yongzhou Hu
Journal:  Eur J Med Chem       Date:  2013-02-09       Impact factor: 6.514

4.  Characterization of the human cysteinyl leukotriene CysLT1 receptor.

Authors:  K R Lynch; G P O'Neill; Q Liu; D S Im; N Sawyer; K M Metters; N Coulombe; M Abramovitz; D J Figueroa; Z Zeng; B M Connolly; C Bai; C P Austin; A Chateauneuf; R Stocco; G M Greig; S Kargman; S B Hooks; E Hosfield; D L Williams; A W Ford-Hutchinson; C T Caskey; J F Evans
Journal:  Nature       Date:  1999-06-24       Impact factor: 49.962

5.  A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice.

Authors:  Nathan C Ni; Dong Yan; Laurel L Ballantyne; Alma Barajas-Espinosa; Tim St Amand; Derek A Pratt; Colin D Funk
Journal:  J Pharmacol Exp Ther       Date:  2011-09-08       Impact factor: 4.030

6.  The cysteinyl-leukotriene receptor antagonist BAY u9773 is a competitive antagonist of leukotriene C4 in the guinea-pig ileum.

Authors:  M Bäck; E W Jonsson; S E Dahlén
Journal:  Eur J Pharmacol       Date:  1996-12-12       Impact factor: 4.432

7.  Expression of cysteinyl leukotriene synthetic and signalling proteins in inflammatory cells in active seasonal allergic rhinitis.

Authors:  D J Figueroa; L Borish; D Baramki; G Philip; C P Austin; J F Evans
Journal:  Clin Exp Allergy       Date:  2003-10       Impact factor: 5.018

Review 8.  Functional characteristics of cysteinyl-leukotriene receptor subtypes.

Authors:  Magnus Bäck
Journal:  Life Sci       Date:  2002-06-28       Impact factor: 5.037

9.  Preparation of benzo[b]furans having five-membered heterocycles at the 2-position and 2-(4-Alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans, and their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity.

Authors:  Yukiko Akai; Yukako Tabuchi; Kumiko Ando; Azusa Ito; Yoko Sakata; Ikuo Kawasaki; Takahiro Ohishi; Masayuki Yamashita; Shunsaku Ohta; Kiyoharu Nishide; Yoshitaka Ohishi
Journal:  Chem Pharm Bull (Tokyo)       Date:  2012       Impact factor: 1.645

10.  Leukotrienes: mediators of immediate hypersensitivity reactions and inflammation.

Authors:  B Samuelsson
Journal:  Science       Date:  1983-05-06       Impact factor: 47.728
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  3 in total

1.  Classification models and SAR analysis on CysLT1 receptor antagonists using machine learning algorithms.

Authors:  Hongzhao Wang; Zijian Qin; Aixia Yan
Journal:  Mol Divers       Date:  2021-02-03       Impact factor: 3.364

2.  Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.

Authors:  Anastasiia Gusach; Aleksandra Luginina; Egor Marin; Rebecca L Brouillette; Élie Besserer-Offroy; Jean-Michel Longpré; Andrii Ishchenko; Petr Popov; Nilkanth Patel; Taku Fujimoto; Toru Maruyama; Benjamin Stauch; Margarita Ergasheva; Daria Romanovskaia; Anastasiia Stepko; Kirill Kovalev; Mikhail Shevtsov; Valentin Gordeliy; Gye Won Han; Vsevolod Katritch; Valentin Borshchevskiy; Philippe Sarret; Alexey Mishin; Vadim Cherezov
Journal:  Nat Commun       Date:  2019-12-06       Impact factor: 14.919

Review 3.  Connections between Immune-Derived Mediators and Sensory Nerves for Itch Sensation.

Authors:  Sumika Toyama; Mitsutoshi Tominaga; Kenji Takamori
Journal:  Int J Mol Sci       Date:  2021-11-16       Impact factor: 5.923
  3 in total

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