title: Resveratrol and related compounds as antioxidants with an allosteric mechanism of action in epigenetic drug targets.
abstract: The present review is intended to focus on naturally occurring cytoprotective agents such as resveratrol (trans-3,4',5-trihydroxystilbene) and other related compounds, probably with similar molecular mechanisms of action and high capacity to find applications in medical fields. Several physiological aspects have been ascribed to resveratrol and similar compounds. Resveratrol, among others, has been recently described as a silent information regulator T1 (SIRT1) activator that increases AMP-activated protein kinase (AMPK) phosphorylation and reduces the oxidative damage biomarkers during aging in laboratory settings. The reports on resveratrol and other SIRT1 activators from various sources are encouraging. The pharmacological strategies for modulation of sirtuins by small molecules through allosteric mechanisms should gain a greater momentum including human research. Resveratrol and resveratrol-like molecules seem to fulfill the requirement of a new horizon in drug research since these molecules cover a growing research means as antioxidants with allosteric mechanism in epigenetic drug targets. However, one should keep in mind the challenges of extrapolation of basic research into clinical results. Overall, the issue of sirtuins in biology and disease provides an insight on therapeutic potentials of sirtuin-based therapeutics and demonstrates the high complexity of drug-targeting these modalities for human applications.
authors.affiliation: Institute of Pharmacology, First Faculty of Medicine, Charles University, Prague, Czech Republic. hassan.farghali@lf1.cuni.cz
authors.forename: H
authors.initials: H
authors.lastname: Farghali
authors.forename: N
authors.initials: N
authors.lastname: Kutinová Canová
authors.forename: N
authors.initials: N
authors.lastname: Lekić
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000378:metabolism; D000494:Allosteric Regulation; D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology*; D004789:Enzyme Activation; D020536:Enzyme Activators / Q000737:chemistry / Q000494:pharmacology*; D044127:Epigenesis, Genetic / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D018384:Oxidative Stress / Q000187:drug effects; D010766:Phosphorylation; D000077185:Resveratrol; D056564:Sirtuin 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D013267:Stilbenes / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000975:Antioxidants; D020536:Enzyme Activators; D013267:Stilbenes; D055372:AMP-Activated Protein Kinases; D056564:Sirtuin 1; D000077185:Resveratrol