Research Peptide · For laboratory research use only
Also known as Glu-Asp-Arg, EDR peptide
Pinealon is the synthetic tripeptide L-glutamyl-L-aspartyl-L-arginine (Glu-Asp-Arg, EDR), one of the short regulatory peptides studied by Khavinson and colleagues in St Petersburg1,7.
The published literature is small and comes almost entirely from that group and its collaborators. It consists of cell culture work (cerebellar granule cells, neutrophils, PC12 cells, ageing cortical cell cultures, HeLa cells and induced neurons), a rat model of prenatal hyperhomocysteinaemia, and biophysical studies of peptide and DNA interaction1,2,3,4,5,6. Independent replication is limited, and the group's review should be read alongside the primary studies7.
As described in the research literature
As described in the research literature, pinealon restricted the accumulation of reactive oxygen species in cerebellar granule cells, neutrophils and PC12 cells exposed to oxidative stress, and reduced necrotic cell death measured by propidium iodide staining; these effects were accompanied by a delayed time course of ERK1/2 activation and by changes in the cell cycle1. Because the cell cycle effects continued at concentrations above those at which the antioxidant effect saturated, the authors proposed that the peptide also interacts directly with the genome1.
Fluorescein-labelled pinealon was observed in the cytoplasm, nucleus and nucleolus of HeLa cells, and fluorescence quenching experiments suggested sequence-preferential binding to deoxyribooligonucleotides3. Spectral, NMR and molecular dynamics work reported that EDR can partly enter the major groove of DNA, with magnesium ions promoting the interaction5. A docking study proposed a complementary site in the tryptophan hydroxylase gene, alongside increased serotonin expression in ageing cortical cell cultures4. These gene-regulation models remain proposals, set out in the group's own review7.
What published studies have examined
Reactive oxygen species accumulation, necrotic cell death, ERK1/2 activation and cell cycle distribution were measured in rat cerebellar granule cells, neutrophils and PC12 cells under receptor-dependent and receptor-independent oxidative stress1.
Sources [1]
Pregnant rats were loaded with dietary methionine to model hyperhomocysteinaemia, and their offspring were examined for spatial orientation and learning, and for reactive oxygen species and necrotic cell numbers in isolated cerebellar neurons2.
Sources [2]
Cellular uptake of labelled short peptides was examined in HeLa cells, with in vitro binding to single- and double-stranded oligonucleotides compared across peptides3. A separate biophysical study used spectroscopy, NMR, viscometry and molecular dynamics to examine EDR binding to DNA and the role of mono- and divalent ions5.
Serotonin expression was examined in ageing cultures of brain cortex cells4. In cortical neurons transdifferentiated from dermal fibroblasts of elderly donors, EDR, KED and AEDG peptides were compared for dendritic arborisation, mitochondrial and lysosomal activity, p16 levels and oxidative DNA damage6.
Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes.
Khavinson V, Ribakova Y, Kulebiakin K, et al. Rejuvenation Research, 2011.
Pinealon protects the rat offspring from prenatal hyperhomocysteinemia.
Arutjunyan A, Kozina L, Stvolinskiy S, et al. International Journal of Clinical and Experimental Medicine, 2012.
Penetration of short fluorescence-labeled peptides into the nucleus in HeLa cells and in vitro specific interaction of the peptides with deoxyribooligonucleotides and DNA.
Fedoreyeva LI, Kireev II, Khavinson VKh, et al. Biochemistry (Moscow), 2011.
Short peptides stimulate serotonin expression in cells of brain cortex.
Khavinson VKh, Lin'kova NS, Tarnovskaya SI, et al. Bulletin of Experimental Biology and Medicine, 2014.
Role of Mono- and Divalent Ions in Peptide Glu-Asp-Arg-DNA Interaction.
Silanteva IA, Komolkin AV, Morozova EA, et al. The Journal of Physical Chemistry B, 2019.
Short Peptides Protect Fibroblast-Derived Induced Neurons from Age-Related Changes.
Kraskovskaya N, Linkova N, Sakhenberg E, et al. International Journal of Molecular Sciences, 2024.
EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer's Disease.
Khavinson V, Linkova N, Kozhevnikova E, et al. Molecules, 2020.
This page is provided for research and educational reference only. It does not constitute medical advice, dosing guidance, or a recommendation for use. All compounds are strictly for laboratory and in-vitro research purposes.