Targeting NRF2–KEAP1 axis by Omega-3 fatty acids and their derivatives: Emerging opportunities against aging and diseases

Davinelli, Sergio; Medoro, Alessandro; Intrieri, Mariano; Saso, Luciano; Scapagnini, Giovanni; Kang, Jing

doi:10.1016/j.freeradbiomed.2022.11.017

Cited by 22 publications

(13 citation statements)

References 182 publications

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“…LBPs can improve the activity of these enzymes to achieve antioxidant effects. Therefore, research on antioxidants provides insights of great import into the prevention and treatment of various redox-related diseases [ 78 ]. In recent years, the antioxidant effects of plant polysaccharides have been widely studied.…”

Section: Molecular Mechanisms Related To the Antioxidant Effect Of Lbpsmentioning

confidence: 99%

Distinct Role of Lycium barbarum L. Polysaccharides in Oxidative Stress-Related Ocular Diseases

et al. 2023

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Oxidative stress is an imbalance between the increased production of reactive species and reduced antioxidant activity, which can cause a variety of disturbances including ocular diseases. Lycium barbarum polysaccharides (LBPs) are complex polysaccharides isolated from the fruit of L. barbarum, showing distinct roles in antioxidants. Moreover, it is relatively safe and non-toxic. In recent years, the antioxidant activities of LBPs have attracted remarkable attention. In order to illustrate its significance and underlying therapeutic value for vision, we comprehensively review the recent progress on the antioxidant mechanisms of LBP and its potential applications in ocular diseases, including diabetic retinopathy, hypertensive neuroretinopathy, age-related macular degeneration, retinitis pigmentosa, retinal ischemia/reperfusion injury, glaucoma, dry eye syndrome, and diabetic cataract.

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Section: Molecular Mechanisms Related To the Antioxidant Effect Of Lbpsmentioning

confidence: 99%

Distinct Role of Lycium barbarum L. Polysaccharides in Oxidative Stress-Related Ocular Diseases

et al. 2023

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“… 390 , 391 , 392 , 393 Recently, a number of small molecules have been shown to modulate the KEAP1/NRF2 axis (Figure 6 ). 284 , 394 , 395 , 396 , 397 , 398 The BTB domain inhibitors, including natural products KEAP1‐1 (a semi‐synthetic oleanolic acid derivative bardoxolone) and KEAP1‐2 (piperlongumine), were discovered as a promising NRF2 modulators utilized in TPD applications by covalently interacting with cysteine residues of KEAP1. 399 On the other hand, a Kelch domain reversible inhibitor, designated as KEAP1 KEAP1‐3, was also discovered as an E3 ligand.…”

Section: Keap1 Ligands and Their Utilizations In Protacsmentioning

confidence: 99%

PROTACs: A novel strategy for cancer drug discovery and development

Han

Sun

2023

MedComm

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Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists of three components: a small molecule that binds to a target protein, an E3 ligase ligand (consisting of an E3 ligase and its small molecule recruiter), and a chemical linker that hooks first two components together. In the past 20 years, we have witnessed advancement of multiple PRO-TAC degraders into the clinical trials for anticancer therapies. However, one of the major challenges of PROTAC technology is that only very limited number of E3 ligase recruiters are currently available as E3 ligand for targeted protein degradation (TPD), although human genome encodes more than 600 E3 ligases. Thus, there is an urgent need to identify additional effective E3 ligase recruiters for TPD applications. In this review, we summarized the existing RING-type E3 ubiquitin ligase and their small molecule recruiters that act as effective E3 ligands of PRO-TAC degraders and their application in anticancer drug discovery. We believe that this review could serve as a reference in future development of efficient E3 ligands of PROTAC technology for cancer drug discovery and development.

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“…Nuclear factor erythroid 2-related factor-2 (Nrf-2), a master transcription factor involved in antioxidant signaling and cell survival responses, regulates a wide battery of cytoprotective responses and protects against pathologies associated with oxidative stress and chronic inflammation such as metabolic, neurodegenerative, and other age-related diseases [ 59 , 101 , 102 ]. Under physiological conditions, Nrf-2 is generally located in the cytoplasm and binds to its inhibitor, Kelch-like ECH-associated protein 1 (Keap1), leading to its degradation.…”

Section: Mechanisms Of Fucoidan Actionsmentioning

confidence: 99%

“…Under physiological conditions, Nrf-2 is generally located in the cytoplasm and binds to its inhibitor, Kelch-like ECH-associated protein 1 (Keap1), leading to its degradation. However, in response to oxidative or electrophilic stress, Nrf-2 dissociates from Keap1 and translocates to the nucleus to bind antioxidant-responsive elements in the promoter regions of its downstream antioxidant genes, including heme oxygenase-1 (HO-1) [ 59 , 101 , 102 ]. Different studies showed that fucoidans diminished oxidative stress and the expression of pro-inflammatory mediators by regulating Nrf2/Keap1 signaling [ 65 , 66 , 92 ].…”

Section: Mechanisms Of Fucoidan Actionsmentioning

confidence: 99%

Relevance of the Extraction Stage on the Anti-Inflammatory Action of Fucoidans

et al. 2023

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The anti-inflammatory action of fucoidans is well known, based on both in vitro and some in vivo studies. The other biological properties of these compounds, their lack of toxicity, and the possibility of obtaining them from a widely distributed and renewable source, makes them attractive novel bioactives. However, fucoidans’ heterogeneity and variability in composition, structure, and properties depending on seaweed species, biotic and abiotic factors and processing conditions, especially during extraction and purification stages, make it difficult for standardization. A review of the available technologies, including those based on intensification strategies, and their influence on fucoidan composition, structure, and anti-inflammatory potential of crude extracts and fractions is presented.

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Targeting NRF2–KEAP1 axis by Omega-3 fatty acids and their derivatives: Emerging opportunities against aging and diseases

Cited by 22 publications

References 182 publications

Distinct Role of Lycium barbarum L. Polysaccharides in Oxidative Stress-Related Ocular Diseases

Distinct Role of Lycium barbarum L. Polysaccharides in Oxidative Stress-Related Ocular Diseases

PROTACs: A novel strategy for cancer drug discovery and development

Relevance of the Extraction Stage on the Anti-Inflammatory Action of Fucoidans

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