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Review

Chemistry of Peptide-Oligonucleotide Conjugates: A Review

1
Faculty of Physics, Novosibirsk State University, 630090 Novosibirsk, Russia
2
Institute of Cytology and Genetics, Russian Academy of Sciences, Siberian Branch, 630090 Novosibirsk, Russia
*
Author to whom correspondence should be addressed.
Academic Editors: Harri Lönnberg and Roger Strömberg
Molecules 2021, 26(17), 5420; https://doi.org/10.3390/molecules26175420
Received: 22 July 2021 / Revised: 30 August 2021 / Accepted: 1 September 2021 / Published: 6 September 2021
(This article belongs to the Special Issue Synthesis and Applications of Oligonucleotide Conjugate II)
Peptide-oligonucleotide conjugates (POCs) represent one of the increasingly successful albeit costly approaches to increasing the cellular uptake, tissue delivery, bioavailability, and, thus, overall efficiency of therapeutic nucleic acids, such as, antisense oligonucleotides and small interfering RNAs. This review puts the subject of chemical synthesis of POCs into the wider context of therapeutic oligonucleotides and the problem of nucleic acid drug delivery, cell-penetrating peptide structural types, the mechanisms of their intracellular transport, and the ways of application, which include the formation of non-covalent complexes with oligonucleotides (peptide additives) or covalent conjugation. The main strategies for the synthesis of POCs are viewed in detail, which are conceptually divided into (a) the stepwise solid-phase synthesis approach and (b) post-synthetic conjugation either in solution or on the solid phase, especially by means of various click chemistries. The relative advantages and disadvantages of both strategies are discussed and compared. View Full-Text
Keywords: cell-penetrating peptide; nucleic acid therapeutic; antisense oligonucleotide; small interfering RNA (siRNA); peptide nucleic acid (PNA); locked nucleic acid (LNA); phosphordiamidate morpholino oligomer (PMO); cellular uptake; drug delivery; click chemistry cell-penetrating peptide; nucleic acid therapeutic; antisense oligonucleotide; small interfering RNA (siRNA); peptide nucleic acid (PNA); locked nucleic acid (LNA); phosphordiamidate morpholino oligomer (PMO); cellular uptake; drug delivery; click chemistry
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MDPI and ACS Style

Klabenkova, K.; Fokina, A.; Stetsenko, D. Chemistry of Peptide-Oligonucleotide Conjugates: A Review. Molecules 2021, 26, 5420. https://doi.org/10.3390/molecules26175420

AMA Style

Klabenkova K, Fokina A, Stetsenko D. Chemistry of Peptide-Oligonucleotide Conjugates: A Review. Molecules. 2021; 26(17):5420. https://doi.org/10.3390/molecules26175420

Chicago/Turabian Style

Klabenkova, Kristina, Alesya Fokina, and Dmitry Stetsenko. 2021. "Chemistry of Peptide-Oligonucleotide Conjugates: A Review" Molecules 26, no. 17: 5420. https://doi.org/10.3390/molecules26175420

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