Difatty Acyl-Conjugated Linear and Cyclic Peptides for siRNA Delivery

ACS Omega
Hung DoHamidreza Montazeri Aliabadi

Abstract

A number of amphiphilic difatty acyl linear and cyclic R5K2 peptide conjugates were synthesized by solid-phase peptide methods to enhance the interaction with the hydrophobic cellular phospholipid bilayer and to improve siRNA delivery and silencing. Binding to siRNA molecules was significantly less for the cyclic peptide conjugates. A gradual decrease was observed in the particle size of the complexes with increasing peptide/siRNA ratio for most of the synthesized peptides, suggesting the complex formation. Most of the complexes showed a particle size of less than 200 nm, which is considered an appropriate size for in vitro siRNA delivery. A number of fatty acyl-conjugated peptides, such as LP-C16 and LP-C18, displayed near complete protection against serum degradation. Flow cytometry studies demonstrated significantly higher internalization of fluorescence-labeled siRNA (FAM-siRNA) in the presence of LP-C16, LP-C18, and CP-C16 with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) addition. Confocal microscopy confirmed the cellular internalization of fluorescence-labeled siRNA in the presence of LP-C16 and LP-C18 with DOPE when compared with cells exposed to DOPE/FAM-siRNA. While C16- and C18-conjugated peptides (especiall...Continue Reading

References

Aug 1, 1995·Proceedings of the National Academy of Sciences of the United States of America·O BoussifJ P Behr
Aug 3, 1999·Journal of Pharmaceutical Sciences·R C Adami, K G Rice
Jan 11, 2005·Journal of Combinatorial Chemistry·Nikos ZinierisNikolas Ferderigos
Jul 11, 2006·Molecular Therapy : the Journal of the American Society of Gene Therapy·Kenneth A HowardJørgen Kjems
Jul 16, 2008·Drug Discovery Today·Koen RaemdonckStefaan C De Smedt
Nov 1, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Anthony J ConvertinePatrick S Stayton
Dec 3, 2008·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Vasiliki Sarli, Athanassios Giannis
Sep 11, 2010·Trends in Pharmacological Sciences·Peter JärverÜlo Langel
Feb 16, 2011·Macromolecular Bioscience·Hamidreza Montazeri AliabadiHasan Uludağ
Jan 3, 2012·Biomaterials·Hamidreza M AliabadiHasan Uludağ
May 4, 2012·Journal of Cellular Physiology·Emanuele MarraLuigi Aurisicchio
Feb 2, 2013·Expert Opinion on Therapeutic Patents·Brian W Dymock, Cheng Shang See
Sep 3, 2013·Journal of Controlled Release : Official Journal of the Controlled Release Society·Hamidreza Montazeri AliabadiHasan Uludağ
Nov 13, 2013·Molecular Pharmaceutics·Amir Nasrolahi ShiraziKeykavous Parang
Apr 15, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Li GuKathryn E Uhrich
Jul 1, 2014·Molecular Pharmaceutics·Donghoon OhKeykavous Parang
Jul 16, 2014·Nature Reviews. Genetics·Hao YinDaniel G Anderson
Aug 30, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Amir Nasrolahi ShiraziKeykavous Parang
Dec 2, 2014·Current Topics in Medicinal Chemistry·Concepción Pérez-Melero
Mar 7, 2015·Biological & Pharmaceutical Bulletin·Yoshiyuki HattoriEtsuo Yonemochi
Jun 19, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·Mehdi RezaeeBizhan Malaekeh-Nikouei
Jun 19, 2016·Biochimie·Elena M SmekalovaVictor Koteliansky
Oct 31, 2016·Advanced Drug Delivery Reviews·Taavi LehtoSamir El Andaloussi
Aug 18, 2016·Advanced Drug Delivery Reviews·Wanyi Tai, Xiaohu Gao
Nov 12, 2016·Methods in Molecular Biology·Vaibhav Saxena
Mar 23, 2017·Molecular Therapy. Nucleic Acids·Yuanyu Huang
Jan 1, 2016·Nanomaterials·Virginia CampaniGiuseppe De Rosa
Apr 9, 2017·Pharmaceutical Research·Ricardo Titze-de-AlmeidaSimoneide Souza Titze-de-Almeida
Sep 4, 2017·Materials Science & Engineering. C, Materials for Biological Applications·Aparna Chaudhary, Sanjeev Garg

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Citations

Apr 20, 2019·Polymers·Saghar MozaffariHamidreza Montazeri Aliabadi
Jan 27, 2021·Molecular Pharmaceutics·Ryley HallHamidreza Montazeri Aliabadi
Jul 23, 2019·Molecular Pharmaceutics·Shang Eun ParkRakesh Kumar Tiwari

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Methods Mentioned

BETA
transfection
dynamic light scattering
electrophoresis
flow cytometry
PCR
electrophoretic mobility shift assay

Software Mentioned

Image J
primer Blast
FlexControl

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