Chemistry of Peptide-Oligonucleotide Conjugates: A Review
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 R...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-09-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/17/5420 |
| _version_ | 1797520984833523712 |
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| author | Kristina Klabenkova Alesya Fokina Dmitry Stetsenko |
| author_facet | Kristina Klabenkova Alesya Fokina Dmitry Stetsenko |
| author_sort | Kristina Klabenkova |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T08:06:12Z |
| format | Article |
| id | doaj.art-bdb958699bcd4d85b2b62697aea99171 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T08:06:12Z |
| publishDate | 2021-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-bdb958699bcd4d85b2b62697aea991712023-11-22T11:03:49ZengMDPI AGMolecules1420-30492021-09-012617542010.3390/molecules26175420Chemistry of Peptide-Oligonucleotide Conjugates: A ReviewKristina Klabenkova0Alesya Fokina1Dmitry Stetsenko2Faculty of Physics, Novosibirsk State University, 630090 Novosibirsk, RussiaFaculty of Physics, Novosibirsk State University, 630090 Novosibirsk, RussiaFaculty of Physics, Novosibirsk State University, 630090 Novosibirsk, RussiaPeptide-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.https://www.mdpi.com/1420-3049/26/17/5420cell-penetrating peptidenucleic acid therapeuticantisense oligonucleotidesmall interfering RNA (siRNA)peptide nucleic acid (PNA)locked nucleic acid (LNA) |
| spellingShingle | Kristina Klabenkova Alesya Fokina Dmitry Stetsenko Chemistry of Peptide-Oligonucleotide Conjugates: A Review Molecules cell-penetrating peptide nucleic acid therapeutic antisense oligonucleotide small interfering RNA (siRNA) peptide nucleic acid (PNA) locked nucleic acid (LNA) |
| title | Chemistry of Peptide-Oligonucleotide Conjugates: A Review |
| title_full | Chemistry of Peptide-Oligonucleotide Conjugates: A Review |
| title_fullStr | Chemistry of Peptide-Oligonucleotide Conjugates: A Review |
| title_full_unstemmed | Chemistry of Peptide-Oligonucleotide Conjugates: A Review |
| title_short | Chemistry of Peptide-Oligonucleotide Conjugates: A Review |
| title_sort | chemistry of peptide oligonucleotide conjugates a review |
| topic | cell-penetrating peptide nucleic acid therapeutic antisense oligonucleotide small interfering RNA (siRNA) peptide nucleic acid (PNA) locked nucleic acid (LNA) |
| url | https://www.mdpi.com/1420-3049/26/17/5420 |
| work_keys_str_mv | AT kristinaklabenkova chemistryofpeptideoligonucleotideconjugatesareview AT alesyafokina chemistryofpeptideoligonucleotideconjugatesareview AT dmitrystetsenko chemistryofpeptideoligonucleotideconjugatesareview |