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

Journal of Medicinal Chemistry
Hélène C BertrandGeoff Wells

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.

References

Mar 30, 2004·Methods in Enzymology·Jed W FaheyPaul Talalay
Mar 30, 2004·Methods in Enzymology·Albena T Dinkova-KostovaPaul Talalay
Oct 12, 2004·The Journal of Biological Chemistry·Xuchu LiLesa J Beamer
Jun 30, 2005·The Journal of Biological Chemistry·Fei HongDaniel C Liebler
Nov 15, 2005·Cancer Epidemiology, Biomarkers & Prevention : a Publication of the American Association for Cancer Research, Cosponsored by the American Society of Preventive Oncology·Thomas W KenslerPaul Talalay
Mar 2, 2006·Molecular Cell·Balasundaram PadmanabhanMasayuki Yamamoto
Aug 5, 2006·Advances in Enzyme Regulation·Makoto Kobayashi, Masayuki Yamamoto
Sep 14, 2006·Annual Review of Pharmacology and Toxicology·Thomas W KenslerShyam Biswal
Nov 4, 2006·Biological Chemistry·Kit I TongMasayuki Yamamoto
Mar 10, 2007·Carcinogenesis·Brian S CornblattKala Visvanathan
Apr 29, 2009·Journal of Computational Chemistry·Garrett M MorrisArthur J Olson
May 8, 2010·Antioxidants & Redox Signaling·John D HayesAlbena T Dinkova-Kostova
Aug 12, 2010·Journal of Medicinal Chemistry·Suresh K TipparajuRima L McLeod
Dec 7, 2010·Experimental and Toxicologic Pathology : Official Journal of the Gesellschaft Für Toxikologische Pathologie·Carlos Enrique Guerrero-BeltránYolanda Irasema Chirino
Mar 3, 2011·Archives of Toxicology·Liam Baird, Albena T Dinkova-Kostova
Nov 24, 2011·Free Radical Biology & Medicine·Rowena HancockGeoff Wells
May 3, 2012·Medicinal Research Reviews·Sadagopan MageshLongqin Hu
May 10, 2012·Journal of Computer-aided Molecular Design·Scott R BrozellRobert C Rizzo
May 15, 2012·ACS Medicinal Chemistry Letters·Richard SteelMark Searcey
May 17, 2012·Journal of Chemical Information and Modeling·John J IrwinRyan G Coleman
Jul 4, 2012·Topics in Current Chemistry·Thomas W KenslerPaul Talalay
Dec 18, 2012·Organic & Biomolecular Chemistry·Antonio Urbano, M Carmen Carreño
Apr 9, 2013·Bioorganic & Medicinal Chemistry Letters·Longqin HuBenito Munoz
Apr 26, 2013·Organic & Biomolecular Chemistry·Rowena HancockGeoff Wells
May 8, 2013·Bioorganic & Medicinal Chemistry·Douglas MarcotteLaura Silvian
Aug 30, 2013·Proceedings of the National Academy of Sciences of the United States of America·Liam BairdAlbena T Dinkova-Kostova
Apr 1, 2014·Biotechnology Advances·Liam BairdAlbena T Dinkova-Kostova
Oct 15, 2014·Proceedings of the National Academy of Sciences of the United States of America·Kanwaljit SinghAndrew W Zimmerman
Dec 3, 2014·Chemistry & Biology·Daniel A EastMichelangelo Campanella

❮ Previous
Next ❯

Citations

Apr 8, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Mostafa M GhorabReem K Arafa
May 19, 2016·Medicinal Research Reviews·Meng-Chen LuQi-Dong You
Sep 30, 2016·The Journal of Organic Chemistry·Isravel MuthukrishnanVellaisamy Sridharan
Apr 30, 2017·Expert Opinion on Therapeutic Patents·Haopeng SunFeng Feng
Mar 24, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Gregory M Rankin, Sally-Ann Poulsen
May 24, 2017·Neurodegenerative Disease Management·Albena T Dinkova-Kostova, Aleksey G Kazantsev
Jul 1, 2017·Annals of the New York Academy of Sciences·Andrey S MarchevMilen I Georgiev
Jun 8, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qing-Ye ZhangHong-Yu Zhang
Jun 22, 2018·Chembiochem : a European Journal of Chemical Biology·Nikolaos D GeorgakopoulosGeoff Wells
Sep 6, 2017·Scientific Reports·Nikolaos D GeorgakopoulosMichelangelo Campanella
Jan 20, 2017·Nature Chemical Biology·Nikolaos D GeorgakopoulosMichelangelo Campanella
Jun 11, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Barbara CosimelliGiampietro Viola
Mar 7, 2018·Pharmacological Reviews·Antonio CuadradoHarald H H W Schmidt
Apr 15, 2020·Molecular and Cellular Biology·Liam Baird, Masayuki Yamamoto
Jun 24, 2020·Open Biology·Sharadha Dayalan Naidu, Albena T Dinkova-Kostova
Jul 19, 2020·Medicinal Research Reviews·Claudia Bento-Pereira, Albena T Dinkova-Kostova
May 7, 2020·Frontiers in Cell and Developmental Biology·Daniela Bakula, Morten Scheibye-Knudsen
Aug 14, 2020·Current Protocols in Toxicology·Dina Dikovskaya, Albena T Dinkova-Kostova
Sep 25, 2020·Signal Transduction and Targeted Therapy·Haiying LuJianyou Shi
May 24, 2017·Proceedings of the National Academy of Sciences of the United States of America·Luisa QuintiAleksey G Kazantsev
May 12, 2020·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Sumi Lee, Longqin Hu
Aug 27, 2017·The Journal of Biological Chemistry·Takafumi Suzuki, Masayuki Yamamoto
Sep 13, 2019·International Journal of Molecular Sciences·Chung-Hang LeungDik-Lung Ma
Sep 6, 2019·Archives of Pharmacal Research·Hye-Youn Cho, Steven R Kleeberger
May 17, 2019·Expert Opinion on Drug Discovery·Xiangyi JiangPeng Zhan
Nov 16, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ashwini Machhindra LondheAe Nim Pae
Jan 6, 2019·Nature Reviews. Drug Discovery·Antonio CuadradoAlbena T Dinkova-Kostova
Aug 10, 2019·Oxidative Medicine and Cellular Longevity·Natalia Robledinos-AntónAntonio Cuadrado
Nov 19, 2019·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Parham Jabbarzadeh KaboliZhangang Xiao
Nov 21, 2020·Antioxidants·Dionysios V ChartoumpekisGerasimos P Sykiotis
Mar 29, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Ibrahim Damilare BoyenleTemitope Isaac Adelusi
Jul 31, 2021·Neurochemistry International·I ŠonskýH Hansíková

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cancer Metabolism

In order for cancer cells to maintain rapid, uncontrolled cell proliferation, they must acquire a source of energy. Cancer cells acquire metabolic energy from their surrounding environment and utilize the host cell nutrients to do so. Here is the latest research on cancer metabolism.