Literature DB >> 26348784

Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction.

Hélène C Bertrand1, Marjolein Schaap1, Liam Baird2, Nikolaos D Georgakopoulos1, Adrian Fowkes1, Clarisse Thiollier1, Hiroko Kachi1, Albena T Dinkova-Kostova2,3, Geoff Wells1.   

Abstract

The transcription factor Nrf2 regulates the expression of a large network of cytoprotective and metabolic enzymes and proteins. Compounds that directly and reversibly inhibit the interaction between Nrf2 and its main negative regulator Keap1 are potential pharmacological agents for a range of disease types including neurodegenerative conditions and cancer. We describe the development of a series of 1,4-diphenyl-1,2,3-triazole compounds that inhibit the Nrf2-Keap1 protein-protein interaction (PPI) in vitro and in live cells and up-regulate the expression of Nrf2-dependent gene products.

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Year:  2015        PMID： 26348784     DOI： 10.1021/acs.jmedchem.5b00602

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  37 in total

1.  Non-covalent NRF2 Activation Confers Greater Cellular Protection than Covalent Activation.

Authors:  Pengfei Liu; Wang Tian; Shasha Tao; Joseph Tillotson; E M Kithsiri Wijeratne; A A Leslie Gunatilaka; Donna D Zhang; Eli Chapman
Journal:  Cell Chem Biol       Date:  2019-08-08       Impact factor: 8.116

Review 2.  Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: a novel approach to activate Nrf2 function.

Authors:  Chunlin Zhuang; Zhongli Wu; Chengguo Xing; Zhenyuan Miao
Journal:  Medchemcomm       Date:  2016-11-17       Impact factor: 3.597

3.  Inhibition of Acinetobacter-Derived Cephalosporinase: Exploring the Carboxylate Recognition Site Using Novel β-Lactamase Inhibitors.

Authors:  Emilia Caselli; Chiara Romagnoli; Rachel A Powers; Magdalena A Taracila; Alexandra A Bouza; Hollister C Swanson; Kali A Smolen; Francesco Fini; Bradley J Wallar; Robert A Bonomo; Fabio Prati
Journal:  ACS Infect Dis       Date:  2017-12-08       Impact factor: 5.084

Review 4.  Stress-sensing mechanisms and the physiological roles of the Keap1-Nrf2 system during cellular stress.

Authors:  Takafumi Suzuki; Masayuki Yamamoto
Journal:  J Biol Chem       Date:  2017-08-24       Impact factor: 5.157

Review 5.  The Molecular Mechanisms Regulating the KEAP1-NRF2 Pathway.

Authors:  Liam Baird; Masayuki Yamamoto
Journal:  Mol Cell Biol       Date:  2020-06-15       Impact factor: 4.272

Review 6.  Mitochondrial biology in airway pathogenesis and the role of NRF2.

Authors:  Hye-Youn Cho; Steven R Kleeberger
Journal:  Arch Pharm Res       Date:  2019-09-04       Impact factor: 4.946

7.  Nrf2 activation through the inhibition of Keap1-Nrf2 protein-protein interaction.

Authors:  Sumi Lee; Longqin Hu
Journal:  Med Chem Res       Date:  2020-04-10       Impact factor: 1.965

8.  Perspectives on the Clinical Development of NRF2-Targeting Drugs.

Authors:  Diego Lastra; Raquel Fernández-Ginés; Gina Manda; Antonio Cuadrado
Journal:  Handb Exp Pharmacol       Date:  2021

9.  KEAP1-modifying small molecule reveals muted NRF2 signaling responses in neural stem cells from Huntington's disease patients.

Authors:  Luisa Quinti; Sharadha Dayalan Naidu; Ulrike Träger; Xiqun Chen; Kimberly Kegel-Gleason; David Llères; Colúm Connolly; Vanita Chopra; Cho Low; Sébastien Moniot; Ellen Sapp; Adelaide R Tousley; Petr Vodicka; Michael J Van Kanegan; Linda S Kaltenbach; Lisa A Crawford; Matthew Fuszard; Maureen Higgins; James R C Miller; Ruth E Farmer; Vijay Potluri; Susanta Samajdar; Lisa Meisel; Ningzhe Zhang; Andrew Snyder; Ross Stein; Steven M Hersch; Lisa M Ellerby; Eranthie Weerapana; Michael A Schwarzschild; Clemens Steegborn; Blair R Leavitt; Alexei Degterev; Sarah J Tabrizi; Donald C Lo; Marian DiFiglia; Leslie M Thompson; Albena T Dinkova-Kostova; Aleksey G Kazantsev
Journal:  Proc Natl Acad Sci U S A       Date:  2017-05-22       Impact factor: 12.779

Review 10.  The potential role of Keap1-Nrf2 pathway in the pathogenesis of Alzheimer's disease, type 2 diabetes, and type 2 diabetes-related Alzheimer's disease.

Authors:  Ling He; Yi Sun
Journal:  Metab Brain Dis       Date:  2021-06-15       Impact factor: 3.584
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