N‐Acylethanolamines Bind to SIRT6

Rahnasto-Rilla, Minna; Kokkola, Tarja; Jarho, Elina; Lahtela‐Kakkonen, Maija; Moaddel, Ruin

doi:10.1002/cbic.201500482

Cited by 38 publications

(45 citation statements)

References 28 publications

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“…The inhibitory activity of resveratrol towards SIRT1 remains controversial, and we can at least say that resveratrol did not greatly affect SIRT activity in our assay system. Quercetin had similar effects on SIRT1 and SIRT6 activities: that is, inhibition at lower concentration, but activation at higher concentration, in accordance with a previous report (Figure D) . Taken together, these results suggest that SIRT modulators generally have similar effects on deacetylase activity and deacylase activity towards long‐chain fatty acyl groups.…”

Section: Resultssupporting

confidence: 92%

A Fluorescent Probe for Imaging Sirtuin Activity in Living Cells, Based on One‐Step Cleavage of the Dabcyl Quencher

et al. 2016

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Sirtuins (SIRTs) are a family of NAD+‐dependent histone deacetylases. In mammals, dysfunction of SIRTs is associated with age‐related metabolic diseases and cancers, so SIRT modulators are considered attractive therapeutic targets. However, current screening methodologies are problematic, and no tools for imaging endogenous SIRT activity in living cells have been available until now. In this work we present a series of simple and highly sensitive new SIRT activity probes. Fluorescence of these probes is activated by SIRT‐mediated hydrolytic release of a 4‐(4‐dimethylaminophenylazo)benzoyl (Dabcyl)‐based FRET quencher moiety from the ϵ‐amino group of lysine in a nonapeptide derived from histone H3K9 and bearing a C‐terminal fluorophore. The probe SFP3 detected activities of SIRT1, ‐2, ‐3, and ‐6, which exhibit deacylase activities towards long‐chain fatty acyl groups. We then truncated the molecular structure of SFP3 in order to improve both its stability to peptidases and its membrane permeability, and developed probe KST‐F, which showed specificity for SIRT1 over SIRT2 and SIRT3. We show that KST‐F can visualize endogenous SIRT1 activity in living cells.

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Section: Resultssupporting

confidence: 92%

A Fluorescent Probe for Imaging Sirtuin Activity in Living Cells, Based on One‐Step Cleavage of the Dabcyl Quencher

et al. 2016

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“…Phenolic compounds, such as quercetin and luteolin, also enhance SIRT6 deacetylation activity, albeit at very high concentrations [13]. …”

Section: Introductionmentioning

confidence: 99%

The Identification of a SIRT6 Activator from Brown Algae Fucus distichus

et al. 2017

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Brown seaweeds contain many bioactive compounds, including polyphenols, polysaccharides, fucosterol, and fucoxantin. These compounds have several biological activities, including anti-inflammatory, hepatoprotective, anti-tumor, anti-hypertensive, and anti-diabetic activity, although in most cases their mechanisms of action are not understood. In this study, extracts generated from five brown algae (Fucus dichitus, Fucus vesiculosus (Linnaeus), Cytoseira tamariscofolia, Cytoseira nodacaulis, Alaria esculenta) were tested for their ability to activate SIRT6 resulting in H3K9 deacetylation. Three of the five macroalgal extracts caused a significant increase of H3K9 deacetylation, and the effect was most pronounced for F. dichitus. The compound responsible for this in vitro activity was identified by mass spectrometry as fucoidan.

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“…Recently, it was reported that NAEs could activate sirtuin 6 in vitro , a NAD + ‐dependent histone deacetylase, which is involved in regulating genomic stability, oxidative stress and glucose metabolism (Rahnasto‐Rilla et al, ). It is at present not known whether this has any physiological or pharmacological significance.…”

Section: Formation and Targets Of N‐acylethanolaminesmentioning

confidence: 99%

Non‐endocannabinoid N‐acylethanolamines and 2‐monoacylglycerols in the intestine

Hansen

Vana

2018

British J Pharmacology

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This review focuses on recent findings of the physiological and pharmacological role of non-endocannabinoid N-acylethanolamines (NAEs) and 2-monoacylglycerols (2-MAGs) in the intestine and their involvement in the gut-brain signalling. Dietary fat suppresses food intake, and much research concerns the known gut peptides, for example, glucagon-like peptide-1 (GLP-1) and cholecystokinin (CCK). NAEs and 2-MAGs represent another class of local gut signals most probably involved in the regulation of food intake. We discuss the putative biosynthetic pathways and targets of NAEs in the intestine as well as their anorectic role and changes in intestinal levels depending on the dietary status. NAEs can activate the transcription factor PPARα, but studies to evaluate the role of endogenous NAEs are generally lacking. Finally, we review the role of diet-derived 2-MAGs in the secretion of anorectic gut peptides via activation of GPR119. Both PPARα and GPR119 have potential as pharmacological targets for the treatment of obesity and the former for treatment of intestinal inflammation.

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N‐Acylethanolamines Bind to SIRT6

Cited by 38 publications

References 28 publications

A Fluorescent Probe for Imaging Sirtuin Activity in Living Cells, Based on One‐Step Cleavage of the Dabcyl Quencher

A Fluorescent Probe for Imaging Sirtuin Activity in Living Cells, Based on One‐Step Cleavage of the Dabcyl Quencher

The Identification of a SIRT6 Activator from Brown Algae Fucus distichus

Non‐endocannabinoid N‐acylethanolamines and 2‐monoacylglycerols in the intestine

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