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Peptides as epigenetic modulators : therapeutic implications

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Abstract
Peptides originating from different sources (endogenous, food derived, environmental, and synthetic) are able to influence different aspects of epigenetic regulation. Endogenous short peptides, resulting from proteolytic cleavage of proteins or upon translation of non-annotated out of frame transcripts, can block DNA methylation and hereby regulate gene expression. Peptides entering the body by digestion of food-related proteins can modulate DNA methylation and/or histone acetylation while environmental peptides, synthesized by bacteria, fungi, and marine sponges, mainly inhibit histone deacetylation. In addition, synthetic peptides that reverse or inhibit different epigenetic modifications of both histones and the DNA can be developed as well. Next to these DNA and histone modifications, peptides can also influence the expression of non-coding RNAs such as lncRNAs and the maturation of miRNAs.Seen the advantages over small molecules, the development of peptide therapeutics is an interesting approach to treat diseases with a strong epigenetic basis like cancer and Alzheimer's disease. To date, only a limited number of drugs with a proven epigenetic mechanism of action have been approved by the FDA of which two (romidepsin and nesiritide) are peptides. A large knowledge gap concerning epigenetic effects of peptides is present, and this class of molecules deserves more attention in the development as epigenetic modulators. In addition, none of the currently approved peptide drugs are under investigation for their potential effects on epigenetics, hampering drug repositioning of these peptides to other indications with an epigenetic etiology.
Keywords
Peptides, Epigenetics, Therapeutical development, Drug repositioning, HISTONE DEACETYLASE INHIBITORS, ATRIAL-NATRIURETIC-PEPTIDE, LONG NONCODING RNA, DNA METHYLATION, GENE-EXPRESSION, DEMETHYLASE 1, SELECTIVE-INHIBITION, ALZHEIMERS-DISEASE, POTENT INHIBITOR, OPIOID-PEPTIDES

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Citation

Please use this url to cite or link to this publication:

MLA
Janssens, Yorick et al. “Peptides as Epigenetic Modulators : Therapeutic Implications.” CLINICAL EPIGENETICS 11 (2019): n. pag. Print.
APA
Janssens, Yorick, Wynendaele, E., Vanden Berghe, W., & De Spiegeleer, B. (2019). Peptides as epigenetic modulators : therapeutic implications. CLINICAL EPIGENETICS, 11.
Chicago author-date
Janssens, Yorick, Evelien Wynendaele, Wim Vanden Berghe, and Bart De Spiegeleer. 2019. “Peptides as Epigenetic Modulators : Therapeutic Implications.” Clinical Epigenetics 11.
Chicago author-date (all authors)
Janssens, Yorick, Evelien Wynendaele, Wim Vanden Berghe, and Bart De Spiegeleer. 2019. “Peptides as Epigenetic Modulators : Therapeutic Implications.” Clinical Epigenetics 11.
Vancouver
1.
Janssens Y, Wynendaele E, Vanden Berghe W, De Spiegeleer B. Peptides as epigenetic modulators : therapeutic implications. CLINICAL EPIGENETICS. 2019;11.
IEEE
[1]
Y. Janssens, E. Wynendaele, W. Vanden Berghe, and B. De Spiegeleer, “Peptides as epigenetic modulators : therapeutic implications,” CLINICAL EPIGENETICS, vol. 11, 2019.
@article{8623442,
  abstract     = {Peptides originating from different sources (endogenous, food derived, environmental, and synthetic) are able to influence different aspects of epigenetic regulation. Endogenous short peptides, resulting from proteolytic cleavage of proteins or upon translation of non-annotated out of frame transcripts, can block DNA methylation and hereby regulate gene expression. Peptides entering the body by digestion of food-related proteins can modulate DNA methylation and/or histone acetylation while environmental peptides, synthesized by bacteria, fungi, and marine sponges, mainly inhibit histone deacetylation. In addition, synthetic peptides that reverse or inhibit different epigenetic modifications of both histones and the DNA can be developed as well. Next to these DNA and histone modifications, peptides can also influence the expression of non-coding RNAs such as lncRNAs and the maturation of miRNAs.Seen the advantages over small molecules, the development of peptide therapeutics is an interesting approach to treat diseases with a strong epigenetic basis like cancer and Alzheimer's disease. To date, only a limited number of drugs with a proven epigenetic mechanism of action have been approved by the FDA of which two (romidepsin and nesiritide) are peptides. A large knowledge gap concerning epigenetic effects of peptides is present, and this class of molecules deserves more attention in the development as epigenetic modulators. In addition, none of the currently approved peptide drugs are under investigation for their potential effects on epigenetics, hampering drug repositioning of these peptides to other indications with an epigenetic etiology.},
  articleno    = {101},
  author       = {Janssens, Yorick and Wynendaele, Evelien and Vanden Berghe, Wim and De Spiegeleer, Bart},
  issn         = {1868-7075},
  journal      = {CLINICAL EPIGENETICS},
  keywords     = {Peptides,Epigenetics,Therapeutical development,Drug repositioning,HISTONE DEACETYLASE INHIBITORS,ATRIAL-NATRIURETIC-PEPTIDE,LONG NONCODING RNA,DNA METHYLATION,GENE-EXPRESSION,DEMETHYLASE 1,SELECTIVE-INHIBITION,ALZHEIMERS-DISEASE,POTENT INHIBITOR,OPIOID-PEPTIDES},
  language     = {eng},
  pages        = {14},
  title        = {Peptides as epigenetic modulators : therapeutic implications},
  url          = {http://dx.doi.org/10.1186/s13148-019-0700-7},
  volume       = {11},
  year         = {2019},
}

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