Literature DB >> 33527033

Targeting microsomal prostaglandin E synthase 1 to develop drugs treating the inflammatory diseases.

Qian Wang1,2, Yuanyuan Li1,2, Mengying Wu1,2, Songming Huang1,2, Aihua Zhang1,2, Yue Zhang1,2, Zhanjun Jia1,2.   

Abstract

Microsomal prostaglandin E synthase 1 (mPGES-1) is the terminal synthase of prostaglandin E2 (PGE2) which plays a crucial role in inflammatory diseases. Thus, mPGES-1 inhibitors are promising agents for their better specificity in blocking the production of PGE2, a potent inflammatory mediator, compared with non-steroidal anti-inflammatory drugs (NSAIDs). Currently, two mPGES-1 inhibitors are undergoing clinical trials and more novel inhibitors are being developed. In this review, we focus on the advances in the development of mPGES-1 inhibitors and the potential of these inhibitors to treat different inflammatory diseases, and discuss the existing challenges. The insights from this review will increase the understanding on the current status of mPGES-1-targeted anti-inflammatory drug development and the potential of these drugs in treating inflammation in diseases. AJTR
Copyright © 2021.

Entities:  

Keywords:  anti-inflammatory drug; inflammation; inhibitor; mPGES-1; prostaglandin E2

Year:  2021        PMID： 33527033      PMCID： PMC7847505     

Source DB:  PubMed          Journal:  Am J Transl Res        ISSN： 1943-8141            Impact factor:   4.060


  107 in total

1.  Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors: SAR and in vivo efficacy in hyperalgesia pain model.

Authors:  Nagarajan Muthukaman; Macchindra Tambe; Mahamadhanif Shaikh; Dnyandeo Pisal; Sanjay Deshmukh; Shital Tondlekar; Neelam Sarode; Lakshminarayana Narayana; Jitendra M Gajera; Vidya G Kattige; Srinivasa Honnegowda; Vikas Karande; Abhay Kulkarni; Dayanidhi Behera; Satyawan B Jadhav; Girish S Gudi; Neelima Khairatkar-Joshi; Laxmikant A Gharat
Journal:  Bioorg Med Chem Lett       Date:  2017-03-24       Impact factor: 2.823

2.  Microglia-specific expression of microsomal prostaglandin E2 synthase-1 contributes to lipopolysaccharide-induced prostaglandin E2 production.

Authors:  Yuri Ikeda-Matsuo; Yuji Ikegaya; Norio Matsuki; Satoshi Uematsu; Shizuo Akira; Yasuharu Sasaki
Journal:  J Neurochem       Date:  2005-07-05       Impact factor: 5.372

3.  Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.

Authors:  Jens Landwehr; Sven George; Eva-Maria Karg; Daniel Poeckel; Dieter Steinhilber; Reinhard Troschuetz; Oliver Werz
Journal:  J Med Chem       Date:  2006-07-13       Impact factor: 7.446

4.  Green tea epigallocatechin-3-gallate inhibits microsomal prostaglandin E(2) synthase-1.

Authors:  Andreas Koeberle; Julia Bauer; Moritz Verhoff; Marika Hoffmann; Hinnak Northoff; Oliver Werz
Journal:  Biochem Biophys Res Commun       Date:  2009-08-06       Impact factor: 3.575

5.  Carnosol and carnosic acids from Salvia officinalis inhibit microsomal prostaglandin E2 synthase-1.

Authors:  Julia Bauer; Susanne Kuehnl; Judith M Rollinger; Olga Scherer; Hinnak Northoff; Hermann Stuppner; Oliver Werz; Andreas Koeberle
Journal:  J Pharmacol Exp Ther       Date:  2012-04-16       Impact factor: 4.030

6.  Microsomal prostaglandin E synthase-1 is a critical factor of stroke-reperfusion injury.

Authors:  Yuri Ikeda-Matsuo; Azusa Ota; Tetsuya Fukada; Satoshi Uematsu; Shizuo Akira; Yasuharu Sasaki
Journal:  Proc Natl Acad Sci U S A       Date:  2006-07-24       Impact factor: 11.205

7.  Identification of key residues determining species differences in inhibitor binding of microsomal prostaglandin E synthase-1.

Authors:  Sven-Christian Pawelzik; Narasimha Rao Uda; Linda Spahiu; Caroline Jegerschöld; Patric Stenberg; Hans Hebert; Ralf Morgenstern; Per-Johan Jakobsson
Journal:  J Biol Chem       Date:  2010-07-06       Impact factor: 5.157

8.  2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors.

Authors:  Simone Di Micco; Carmela Spatafora; Nunzio Cardullo; Raffaele Riccio; Katrin Fischer; Carlo Pergola; Andreas Koeberle; Oliver Werz; Malik Chalal; Dominique Vervandier-Fasseur; Corrado Tringali; Giuseppe Bifulco
Journal:  Bioorg Med Chem       Date:  2016-01-04       Impact factor: 3.641

9.  Microsomal prostaglandin E synthase-1 is induced in alzheimer's disease and its deletion mitigates alzheimer's disease-like pathology in a mouse model.

Authors:  Yoshiharu Akitake; Yoshihito Nakatani; Daisuke Kamei; Masato Hosokawa; Hiroyasu Akatsu; Satoshi Uematsu; Shizuo Akira; Ichiro Kudo; Shuntaro Hara; Mitsuo Takahashi
Journal:  J Neurosci Res       Date:  2013-03-29       Impact factor: 4.164

10.  Structure-based discovery of mPGES-1 inhibitors suitable for preclinical testing in wild-type mice as a new generation of anti-inflammatory drugs.

Authors:  Kai Ding; Ziyuan Zhou; Shurong Hou; Yaxia Yuan; Shuo Zhou; Xirong Zheng; Jianzhong Chen; Charles Loftin; Fang Zheng; Chang-Guo Zhan
Journal:  Sci Rep       Date:  2018-03-26       Impact factor: 4.379
View more
  1 in total

1.  Latest progress in the development of cyclooxygenase-2 pathway inhibitors targeting microsomal prostaglandin E2 synthase-1.

Authors:  Krista LaBorde; Renzhong Lu; Ke-He Ruan
Journal:  Future Med Chem       Date:  2022-01-05       Impact factor: 3.808
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.