2024

TRP14 is the rate limiting enzyme for intracellular cystine reduction and regulates proteome cysteinylation. EMBO Journal. Accepted 2024. DOI: 10.1038/s44318-024-00117-1

The mitochondrial Na+/Ca2+ exchanger NCLX is implied in the activation of hypoxia-inducible factors. Redox Biol. Nov 2024. 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. Sept 2024. 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. Aug 2024. DOI: 10.1016/j.ejmech.2024.116763

Biomarkers of NRF2 signalling: Current status and future challenges. Redox Biol. Jun 2024. 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. May 2024. DOI: 10.1016/j.redox.2024.103117

Innovative pathological network-based multitarget approaches for Alzheimer’s disease treatment. Med Res Rev. Apr 2024. DOI: 10.1002/med.22045

Adipose tissue as a therapeutic target for vascular damage in Alzheimer’s disease. Br J Pharmacol. Mar 2024. DOI: 10.1111/bph.16243

Specific targeting of the NRF2/β-TrCP axis promotes beneficial effects in NASH. Redox Biol. Feb 2024. 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. Jan 2024. DOI: 10.1124/jpet.123.001586

2023

Drug repurposing on Alzheimer’s disease through modulation of NRF2 neighborhood. Redox Biol. Nov 2023. DOI: 10.1016/j.redox.2023.102881

Redox regulation of microglial inflammatory response: Fine control of NLRP3 inflammasome through Nrf2 and NOX4. Antioxidants (Basel). Sep 2023. DOI: 10.3390/antiox12091729

Adipose tissue as a therapeutic target for vascular damage in Alzheimer’s disease. Br J Pharmacol. Sep 2023. DOI: 10.1111/bph.16243

Mechanisms of NURR1 regulation: consequences for its biological activity and involvement in pathology. Int J Mol Sci. Jul 2023. DOI: 10.3390/ijms241512280

Personalized redox medicine in inflammatory bowel diseases: an emerging role for HIF-1α and NRF2 as therapeutic targets. Redox Biol. Apr 2023. DOI: 10.1016/j.redox.2023.102603

The transcription factor NRF2 has epigenetic regulatory functions modulating HDACs, DNMTs, and miRNA biogenesis. Antioxidants. Mar 2023. 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. Feb 2023. 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. Feb 2023. DOI: 10.1016/j.freeradbiomed.2022.12.100

Small synthetic hyaluronan disaccharide BIS014 mitigates neuropathic pain in mice. J Pain. Jan 2023. DOI: 10.1016/j.jpain.2022.07.014

Cytotoxicity models in chromaffin cells to evaluate neuroprotective compounds. Methods Mol Biol.  2023. 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. Dec 2022. 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. Nov 2022. DOI: 10.1016/j.freeradbiomed.2022.09.023

Overlooked and valuable facts to know in the NRF2/KEAP1 field. Free Radic Biol Med. Nov 2022. DOI: 10.1016/j.freeradbiomed.2022.08.044

Microglial Hemoxygenase-1 deletion reduces inflammation in the retina of old mice with tauopathy. Antioxidants (Basel). Oct 2022. DOI: 10.3390/antiox11112151

Dipeptide repeat pathology in c9orf72-ALS is associated with redox, mitochondrial and NRF2 pathway imbalance. Antioxidants (Basel). Sep 2022. 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. Oct 2022. DOI:10.1021/acs.jmedchem.2c00515

Pros and cons of NRF2 activation as adjunctive therapy in rheumatoid arthritis. Free Radic Biol Med. Sep 2022. 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. Sep 2022. DOI: 10.1016/j.redox.2022.102396

KEAP1-NRF2 protein–protein interaction inhibitors: Design, pharmacological properties and therapeutic potential. Medicinal Research Reviews.  Sep 2022. 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. Jul 2022. DOI: 10.1016/j.freeradbiomed.2022.05.016

Loss of KEAP1 causes an accumulation of nondegradative organelles. Antioxidants (Basel). Jul 2022. DOI: 10.3390/antiox11071398

Brain-protective mechanisms of transcription factor NRF2: toward a common strategy for neurodegenerative diseases. Annu Rev Pharmacol Toxicol. 2022. 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.  Jun 2022. 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. May 2022. DOI: http://10.3390/antiox11050946

Novel series of dual NRF2 inducers and selective MAO-B inhibitors for the treatment of Parkinson’s disease. Antioxidants. Feb 2022. DOI: http://10.3390/antiox11020247 

Implication of type 4 NADPH oxidase (NOX4) in tauopathy. Redox Biology. Feb 2022. 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. 2022. 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. 2022. 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. Jan 2022. DOI: http://10.3390/antiox11010028

Enantioselective synthesis and pharmacological evaluation of AZA-CGP37157-Lipoic Acid hybrids for the treatment of Alzheimer’s disease. Antioxidants (Basel). Jan 2022. 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. Apr. 2021. DOI: 10.3390/molecules26082107

Acetylated tau inhibits chaperone-mediated autophagy and promotes tau pathology propagation in mice. Nature Communcations. Dec 2021. 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. Jun 2021. DOI: http://10.3390/antiox10060941

Cannabinoid receptor CB2 ablation protects against TAU induced neurodegeneration. Acta Neuropathol Commun. May 2021. 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. Sep 2021. 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.  Nov  2021. DOI:http://10.1016/j.neulet.2021.136275

Enhanced stability and bioactivity of natural anticancer topoisomerase i inhibitors through cyclodextrin complexation. Pharmaceutics. Oct 2021. DOI: http://10.3390/pharmaceutics13101609

α-Synuclein Induces the GSK-3-Mediated Phosphorylation and Degradation of NURR1 and Loss of Dopaminergic Hallmarks. Molecular Neurobiology. Dec  2021. 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. Chem. 2021. 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. Jan 2021. 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. Dec 2020. 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. Feb 2020. DOI: 10.1016/j.phrs.2019.104597

Nordihydroguaiaretic Acid: From Herbal Medicine to Clinical Development for Cancer and Chronic Diseases. Frontiers in  Pharmacology. Feb 2020. 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. Mar 2020. 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. May 2020. 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. May 2020. DOI: 10.1002/ddr.21618

NRF2 Regulation Processes as a Source of Potential Drug Targets against Neurodegenerative Diseases. Biomolecules. Jun 2020. DOI: 10.3390/biom10060904

Aging and Progression of Beta-Amyloid Pathology in Alzheimer’s Disease Correlates with Microglial Heme-Oxygenase-1 Overexpression. Antioxidants. Jul 2020. DOI: 10.3390/antiox9070644

Na+ controls hypoxic signalling by the mitochondrial respiratory chain. Nature. Jul 2020. 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. Aug 2020. DOI: 

When It Comes to an End: Oxidative Stress Crosstalk with Protein Aggregation and Neuroinflammation Induce Neurodegeneration. Antioxidants. Aug 2020. DOI: 10.3390/antiox9080740 

Protective role of microglial HO-1 blockade in aging: Implication of iron metabolism. Redox Biology. Nov 2020. DOI: 10.1016/j.redox.2020.101789

Wip modulates oxidative stress through NRF2/KEAP1 in glioblastoma cells. Antioxidants. Sep. 2020. DOI: http://10.3390/antiox9090773

Can Activation of NRF2 Be a Strategy against COVID-19?Antioxidants. Trends in Pharmacological Sciences. Sep. 2020. DOI: 10.1016/j.tips.2020.07.003

Perspectives on the Clinical Development of NRF2-Targeting Drugs. Handbook of Experimental Pharmacology (Chapter). Aug 2020. 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. 2020. DOI: http://10.33594/000000210

2019

Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases. Nat Rev Drug Discov. Jan 2019. 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. Mar 2019. DOI: 10.1080/14756366.2019.1581184  

Activators and Inhibitors of NRF2: A Review of Their Potential for Clinical Development. Oxid Med Cell Longev. Jul 2019. 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. Aug 2019. DOI: http://10.1111/jpi.12578

2018

Pharmacological targeting of GSK-3 and NRF2 provides neuroprotection in a preclinical model of tauopathy. Redox Biol. Apr 2018. 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. 2018. 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. April 2018. DOI:10.1124/pr.117.014753

Transcription factor NFE2L2/NRF2 modulates chaperone-mediated autophagy through the regulation of LAMP2A. Autophagy. Jul 2018. 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. Sep 2018. 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. Oct 2018. DOI: 10.1016/j.ejmech.2018.07.056