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Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases.
Cuadrado, Antonio; Rojo, Ana I; Wells, Geoffrey; Hayes, John D; Cousin, Sharon P; Rumsey, William L; Attucks, Otis C; Franklin, Stephen; Levonen, Anna-Liisa; Kensler, Thomas W; Dinkova-Kostova, Albena T.
Afiliación
  • Cuadrado A; Centro de Investigación Biomédica en Red Sobre Enfermedades Neurodegenerativas (CIBERNED), Instituto de Investigación Sanitaria La Paz (IdiPaz), Department of Biochemistry and Instituto de Investigaciones Biomédicas Alberto Sols UAM-CSIC, Faculty of Medicine, Autonomous University of Madrid, Madrid,
  • Rojo AI; Victor Babes National Institute of Pathology, Bucharest, Romania.
  • Wells G; Centro de Investigación Biomédica en Red Sobre Enfermedades Neurodegenerativas (CIBERNED), Instituto de Investigación Sanitaria La Paz (IdiPaz), Department of Biochemistry and Instituto de Investigaciones Biomédicas Alberto Sols UAM-CSIC, Faculty of Medicine, Autonomous University of Madrid, Madrid,
  • Hayes JD; Victor Babes National Institute of Pathology, Bucharest, Romania.
  • Cousin SP; UCL School of Pharmacy, University College London, London, UK.
  • Rumsey WL; Jacqui Wood Cancer Centre, Division of Cellular Medicine, School of Medicine, University of Dundee, Dundee, Scotland, UK.
  • Attucks OC; Reata Pharmaceuticals, Irving, TX, USA.
  • Franklin S; GlaxoSmithKline, Collegeville, PA, USA.
  • Levonen AL; vTv Therapeutics, High Point, NC, USA.
  • Kensler TW; Evgen Pharma, Wilmslow, Cheshire, UK.
  • Dinkova-Kostova AT; A. I. Virtanen Institute for Molecular Sciences, University of Eastern Finland, Kuopio, Finland.
Nat Rev Drug Discov ; 18(4): 295-317, 2019 04.
Article en En | MEDLINE | ID: mdl-30610225
ABSTRACT
The transcription factor NF-E2 p45-related factor 2 (NRF2; encoded by NFE2L2) and its principal negative regulator, the E3 ligase adaptor Kelch-like ECH-associated protein 1 (KEAP1), are critical in the maintenance of redox, metabolic and protein homeostasis, as well as the regulation of inflammation. Thus, NRF2 activation provides cytoprotection against numerous pathologies including chronic diseases of the lung and liver; autoimmune, neurodegenerative and metabolic disorders; and cancer initiation. One NRF2 activator has received clinical approval and several electrophilic modifiers of the cysteine-based sensor KEAP1 and inhibitors of its interaction with NRF2 are now in clinical development. However, challenges regarding target specificity, pharmacodynamic properties, efficacy and safety remain.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Quimioterapia / Factor 2 Relacionado con NF-E2 / Proteína 1 Asociada A ECH Tipo Kelch Límite: Animals / Humans Idioma: En Revista: Nat Rev Drug Discov Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2019 Tipo del documento: Article
Texto completo
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Quimioterapia / Factor 2 Relacionado con NF-E2 / Proteína 1 Asociada A ECH Tipo Kelch Límite: Animals / Humans Idioma: En Revista: Nat Rev Drug Discov Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2019 Tipo del documento: Article