2025

Network-based drug optimization toward the treatment of Parkinson's disease: NRF2, MAO-B, oxidative stress, and chronic neuroinflammation

Journal of Medicinal chemistry. DOI: 10.1021/acs.jmedchem.4c02659

 

Exploring the broad-spectrum activity of carbohydrate-based Iberin analogues: From anticancer effect to antioxidant properties

European Journal of Medicinal Chemistry. DOI: 10.1016/j.ejmech.2025.117469

 

NRF2 activation by 6-MSITC increases the generation of neuroprotective, soluble alpha-amyloid precursor protein by inducing the metalloprotease gene ADAM17

Free Radical Biology in Medicine. DOI: 10.1016/j.freeradbiomed.2024.11.048

 

Proteostasis decline and redox imbalance in age-related diseases: The therapeutic potential of NRF2.

Biomolecules. DOI: 10.3390/biom15010113

 

Health position paper and redox perspectives - Bench to bedside transition for pharmacological regulation of NRF2 in noncommunicable diseases.

Redox Biology. DOI: 10.1016/j.redox.2025.103569

 

Model organisms for investigating the functional involvement of NRF2 in non-communicable diseases.

Redox Biology. DOI: 10.1016/j.redox.2024.103464

2024

TRP14 is the rate limiting enzyme for intracellular cystine reduction and regulates proteome cysteinylation.

EMBO Journal. DOI: 10.1038/s44318-024-00117-1

 

The mitochondrial Na+/Ca2+ exchanger NCLX is implied in the activation of hypoxia-inducible factors.

Redox Biol. DOI: 10.1016/j.redox.2024.103364

 

The NRF2 inducer CDDO-2P-Im provokes a reduction in amyloid? Levels in Alzheimer’s disease model mice.

 J Biochem. DOI: 10.1093/jb/mvae060

 

Discovery of a potent melatonin-based inhibitor of quinone reductase-2 with neuroprotective and neurogenic properties.

Eur J Med Chem. DOI: 10.1016/j.ejmech.2024.116763

 

Biomarkers of NRF2 signalling: Current status and future challenges.

Redox Biol. DOI: 10.1016/j.redox.2024.103134

 

Inhibition of glycogen synthase kinase-3 enhances NRF2 protein stability, nuclear localisation and target gene transcription in pancreatic beta cells.

Redox Biol. DOI: 10.1016/j.redox.2024.103117

 

Innovative pathological network-based multitarget approaches for Alzheimer’s disease treatment.

Med Res Rev. DOI: 10.1002/med.22045

 

Adipose tissue as a therapeutic target for vascular damage in Alzheimer’s disease.

Br J Pharmacol. DOI: 10.1111/bph.16243

 

Specific targeting of the NRF2/β-TrCP axis promotes beneficial effects in NASH.

Redox Biol. DOI: 10.1016/j.redox.2024.103027

 

The Melatonin Derivative ITH13001 Prevents Hypertension and Cardiovascular Alterations in Angiotensin II-Infused mice.

 J Pharmacol Exp Ther. DOI: 10.1124/jpet.123.001586

2023

Drug repurposing on Alzheimer’s disease through modulation of NRF2 neighborhood.

Redox Biol. DOI: 10.1016/j.redox.2023.102881

 

Redox regulation of microglial inflammatory response: Fine control of NLRP3 inflammasome through Nrf2 and NOX4.

Antioxidants. DOI: 10.3390/antiox12091729

 

Adipose tissue as a therapeutic target for vascular damage in Alzheimer’s disease.

Br J Pharmacol. DOI: 10.1111/bph.16243

 

Mechanisms of NURR1 regulation: consequences for its biological activity and involvement in pathology.

Int J Mol Sci. DOI: 10.3390/ijms241512280

 

Personalized redox medicine in inflammatory bowel diseases: an emerging role for HIF-1α and NRF2 as therapeutic targets.

Redox Biol. DOI: 10.1016/j.redox.2023.102603

 

The transcription factor NRF2 has epigenetic regulatory functions modulating HDACs, DNMTs, and miRNA biogenesis.

Antioxidants. DOI: 10.3390/antiox12030641

 

8-Amide and 8-carbamate substitution patterns as modulators of 7-hydroxy-4-methylcoumarin’s antidepressant profile: synthesis, biological evaluation and docking studies.

Eur. J. Med. Chem. DOI: 10.1016/j.ejmech.2023.115091

 

Introduction to special issue on «Bench to bedside transition for pharmacological regulation of NRF2 in noncommunicable diseases».

Free Radic Biol Med. DOI: 10.1016/j.freeradbiomed.2022.12.100

 

Small synthetic hyaluronan disaccharide BIS014 mitigates neuropathic pain in mice.

J Pain. DOI: 10.1016/j.jpain.2022.07.014

 

Cytotoxicity models in chromaffin cells to evaluate neuroprotective compounds.

Methods Mol Biol. DOI:https://pubmed.ncbi.nlm.nih.gov/36205906/https://doi.org/10.1002/med.21925

2022

Impairment in novelty-promoted memory via behavioral tagging and capture before apparent memory loss in a knock-in model of Alzheimer’s disease.

Sci Rep. DOI: 10.1038/s41598-022-26113-1

 

The current status and future prospects for therapeutic targeting of KEAP1-NRF2 and β-TrCP-NRF2 interactions in cancer chemoresistance.

Free Radic Biol Med. DOI: 10.1016/j.freeradbiomed.2022.09.023

 

Overlooked and valuable facts to know in the NRF2/KEAP1 field.

Free Radic Biol Med. DOI: 10.1016/j.freeradbiomed.2022.08.044

 

Microglial Hemoxygenase-1 deletion reduces inflammation in the retina of old mice with tauopathy.

Antioxidants. DOI: 10.3390/antiox11112151

 

Dipeptide repeat pathology in c9orf72-ALS is associated with redox, mitochondrial and NRF2 pathway imbalance.

Antioxidants. DOI: 10.3390/antiox11101897

 

Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.

 J Med Chem. DOI:10.1021/acs.jmedchem.2c00515

 

Pros and cons of NRF2 activation as adjunctive therapy in rheumatoid arthritis.

Free Radic Biol Med. DOI: 10.1016/j.freeradbiomed.2022.08.012

 

An inhibitor of interaction between the transcription factor NRF2 and the E3 ubiquitin ligase adapter β-TrCP delivers anti-inflammatory responses in mouse liver.

Redox Biol. DOI: 10.1016/j.redox.2022.102396

 

KEAP1-NRF2 protein–protein interaction inhibitors: Design, pharmacological properties and therapeutic potential.

Medicinal Research Reviews. DOI:https://doi.org/10.1002/med.21925

 

Protective actions of nuclear factor erythroid 2-related factor 2 (NRF2) and downstream pathways against environmental stressors.

Free Radic Biol Med. DOI: 10.1016/j.freeradbiomed.2022.05.016

 

Loss of KEAP1 causes an accumulation of nondegradative organelles.

Antioxidants. DOI: 10.3390/antiox11071398

 

Brain-protective mechanisms of transcription factor NRF2: toward a common strategy for neurodegenerative diseases.

Annu Rev Pharmacol Toxicol. DOI: http://10.1146/annurev-pharmtox-052220-103416

 

Antinociceptive and modulatory effect of pathoplastic changes in spinal glia of a TLR4 /CD14 blocking molecule in two models of pain in rat.

Biomed Pharmacother. DOI: 10.1016/j.biopha.2022.112986

 

Transcription factor NRF2 participates in cell cycle progression at the level of G1/S and mitotic checkpoints.

Antioxidants. DOI: http://10.3390/antiox11050946

 

Novel series of dual NRF2 inducers and selective MAO-B inhibitors for the treatment of Parkinson’s disease.

Antioxidants. DOI: http://10.3390/antiox11020247 

 

Implication of type 4 NADPH oxidase (NOX4) in tauopathy.

Redox Biology. DOI: 10.1016/j.redox.2021.102210

 

Antinociceptive and modulatory effect of pathoplastic changes in spinal glia of a TLR4/CD14 blocking molecule in two models of pain in rat.

Biomed. Pharmacother. DOI: https://doi.org/10.1016/j.biopha.2022.112986

 

Resveratrol-based MTDLs to stimulate defensive and regenerative pathways and block early events in neurodegenerative cascades.

J. Med. Chem. DOI: https://doi.org/10.1021/acs.jmedchem.1c01883

 

Curcumin-piperlongumine hybrids with a multitarget profile elicit neuroprotection in in vitro models of oxidative stress and hyperphosphorylation.

Antioxidants. DOI: http://10.3390/antiox11010028

 

Enantioselective synthesis and pharmacological evaluation of AZA-CGP37157-Lipoic Acid hybrids for the treatment of Alzheimer’s disease.

Antioxidants. DOI: 10.3390/antiox11010112

2021

Central Activation of Alpha7 Nicotinic Signaling Attenuates LPS-Induced Neuroinflammation and Sickness Behavior in Adult but Not in Aged Animals.

Molecules. DOI: 10.3390/molecules26082107

 

Acetylated tau inhibits chaperone-mediated autophagy and promotes tau pathology propagation in mice.

Nature Communcations. DOI:http://10.1038/s41467-021-22501-9

 

Bisavenathramide analogues as nrf2 inductors and neuroprotectors in in vitro models of oxidative stress and hyperphosphorylation.

Antioxidants. DOI: http://10.3390/antiox10060941

 

Cannabinoid receptor CB2 ablation protects against TAU induced neurodegeneration.

Acta Neuropathol Commun. DOI: http://10.1186/s40478-021-01196-5

 

NRF2 as a therapeutic opportunity to impact in the molecular roadmap of ALS.

Free Radical Biology and Medicine. DOI: http://10.1016/j.freeradbiomed.2021.07.022

 

Intracellular calcium and inflammatory markers, mediated by purinergic stimulation, are differentially regulated in monocytes of patients with major depressive disorder.

Neuroscience Letters. DOI:http://10.1016/j.neulet.2021.136275

 

Enhanced stability and bioactivity of natural anticancer topoisomerase i inhibitors through cyclodextrin complexation.

Pharmaceutics. DOI: http://10.3390/pharmaceutics13101609

 

α-Synuclein Induces the GSK-3-Mediated Phosphorylation and Degradation of NURR1 and Loss of Dopaminergic Hallmarks.

Molecular Neurobiology. DOI: http://10.1007/s12035-021-02558-9

 

Synthesis and in vitro study of nitro- and methoxy-2-phenylbenzofurans as human monoamine oxidase inhibitors.

Bioorg. DOI: https://doi.org/10.1016/j.bioorg.2020.104616

 

Protective role of microglial HO-1 blockade in aging: implication of iron metabolism.

Redox Biology. DOI: 10.1016/j.redox.2020.101789

 

2020

Cognitive enhancement, tau phosphorylation reduction and neuronal protection by the treatment of a LRRK2 inhibitor in a taoupathy mouse model. 

Neurobiology of Aging. DOI: 10.1016/j.neurobiolaging.2020.09.006

 

Melatonin-sulforaphane hybrid ITH12674 attenuates glial response in vivo by blocking LPS binding to MD2 and receptor oligomerization.

Pharmacological Research. DOI: 10.1016/j.phrs.2019.104597

 

Nordihydroguaiaretic Acid: From Herbal Medicine to Clinical Development for Cancer and Chronic Diseases.

Frontiers in  Pharmacology. DOI: http://10.3389/fphar.2020.00151

 

Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties.

Eur. J. Med. Chem. DOI: 10.1016/j.ejmech.2020.112090

 

Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups.

Eur. J. Med. Chem. DOI: 10.1016/j.ejmech.2020.112403

 

Aza-CGP37157-lipoic hybrids designed as novel Nrf2-inducers and antioxidants exert neuroprotection against oxidative stress and show neuroinflammation inhibitory properties.

Drug Development Research. DOI: 10.1002/ddr.21618

 

NRF2 Regulation Processes as a Source of Potential Drug Targets against Neurodegenerative Diseases.

Biomolecules. DOI: 10.3390/biom10060904

 

Aging and Progression of Beta-Amyloid Pathology in Alzheimer’s Disease Correlates with Microglial Heme-Oxygenase-1 Overexpression.

Antioxidants. DOI: 10.3390/antiox9070644

 

Na+ controls hypoxic signalling by the mitochondrial respiratory chain.

Nature. DOI 10.1038/s41586-020-2551-y

 

Antioxidant, anti-inflammatory and neuroprotective profiles of novel 1,4-dihydropyridine derivatives for the treatment of Alzheimer’s disease.

Antioxidants. DOI: 0.3390/antiox9080650

 

When It Comes to an End: Oxidative Stress Crosstalk with Protein Aggregation and Neuroinflammation Induce Neurodegeneration.

Antioxidants. DOI: 10.3390/antiox9080740 

 

Protective role of microglial HO-1 blockade in aging: Implication of iron metabolism.

Redox Biology. DOI: 10.1016/j.redox.2020.101789

 

Wip modulates oxidative stress through NRF2/KEAP1 in glioblastoma cells.

Antioxidants. DOI: http://10.3390/antiox9090773

 

Can Activation of NRF2 Be a Strategy against COVID-19?

Trends in Pharmacological Sciences. DOI: 10.1016/j.tips.2020.07.003

 

Perspectives on the Clinical Development of NRF2-Targeting Drugs.

Handbook of Experimental Pharmacology (Chapter). DOI: 10.1007/164_2020_381

 

New Nrf2-inducer compound ITH12674 slows the progression of retinitis pigmentosa in the mouse model rd10.

Cellular Physiology And Biochemistry. DOI: http://10.33594/000000210

2019

Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases.

Nat Rev Drug Discov. DOI: 10.1038/s41573-018-0008-

 

New flavonoid – N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic properties.

J. Enzyme Inhib. Med. Chem. DOI: 10.1080/14756366.2019.1581184  

 

Activators and Inhibitors of NRF2: A Review of Their Potential for Clinical Development.

Oxid Med Cell Longev. DOI: 10.1155/2019/9372182

 

Pharmacological doses of melatonin impede cognitive decline in tau-related Alzheimer models, once tauopathy is initiated, by restoring the autophagic flux.

Journal of Pineal research. DOI: http://10.1111/jpi.12578

Pharmacological targeting of GSK-3 and NRF2 provides neuroprotection in a preclinical model of tauopathy.

Redox Biol. DOI: 10.1016/j.redox.2017.10.010

 

Neurogenic and neuroprotective donepezil-flavonoid hybrids wit sigma-1 affinity and inhibition of key enzymes in Alzheimer’s disease.

Eur. J. Med. Chem. DOI: https://doi.org/10.1016/j.ejmech.2018.07.026

 

Transcription Factor NRF2 as a Therapeutic Target for Chronic Diseases: A Systems Medicine Approach.

Pharmacol Rev. DOI:10.1124/pr.117.014753

 

Transcription factor NFE2L2/NRF2 modulates chaperone-mediated autophagy through the regulation of LAMP2A.

Autophagy. DOI: 10.1080/15548627.2018.1474992

 

Deficiency in the transcription factor NRF2 worsens inflammatory parameters in a mouse model with combined tauopathy and amyloidopathy.

Redox Biol. DOI: 10.1016/j.redox.2018.07.006

 

Multi-target-directed ligands for Alzheimer´s disease: discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.

Eur. J. Med. Chem. DOI: 10.1016/j.ejmech.2018.07.056

2018

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