Targeting NRF2 and its downstream processes: opportunities and challenges
L Torrente, GM DeNicola - Annual review of pharmacology and …, 2022 - annualreviews.org
Annual review of pharmacology and toxicology, 2022•annualreviews.org
The transcription factor NRF2 coordinates the expression of a vast array of cytoprotective
and metabolic genes in response to various stress inputs to restore cellular homeostasis.
Transient activation of NRF2 in healthy tissues has been long recognized as a cellular
defense mechanism and is critical to prevent cancer initiation by carcinogens. However,
cancer cells frequently hijack the protective capability of NRF2 to sustain the redox balance
and meet their metabolic requirements for proliferation. Further, aberrant activation of NRF2 …
and metabolic genes in response to various stress inputs to restore cellular homeostasis.
Transient activation of NRF2 in healthy tissues has been long recognized as a cellular
defense mechanism and is critical to prevent cancer initiation by carcinogens. However,
cancer cells frequently hijack the protective capability of NRF2 to sustain the redox balance
and meet their metabolic requirements for proliferation. Further, aberrant activation of NRF2 …
The transcription factor NRF2 coordinates the expression of a vast array of cytoprotective and metabolic genes in response to various stress inputs to restore cellular homeostasis. Transient activation of NRF2 in healthy tissues has been long recognized as a cellular defense mechanism and is critical to prevent cancer initiation by carcinogens. However, cancer cells frequently hijack the protective capability of NRF2 to sustain the redox balance and meet their metabolic requirements for proliferation. Further, aberrant activation of NRF2 in cancer cells confers resistance to commonly used chemotherapeutic agents and radiotherapy. During the last decade, many research groups have attempted to block NRF2 activity in tumors to counteract the survival and proliferative advantage of cancer cells and reverse resistance to treatment. In this review, we highlight the role of NRF2 in cancer progression and discuss the past and current approaches to disable NRF2 signaling in tumors.
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