Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides
In this review, we discuss emerging technologies for drug discovery, which yields novel molecular scaffolds based on natural product-inspired non-traditional peptides expressed using the translation machinery. Unlike natural products, these technologies allow for constructing mRNA-encoding libraries...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2013-03-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1420-3049/18/3/3502 |
| _version_ | 1818117448766849024 |
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| author | Hiroaki Suga Toby Passioura Kenichiro Ito |
| author_facet | Hiroaki Suga Toby Passioura Kenichiro Ito |
| author_sort | Hiroaki Suga |
| collection | DOAJ |
| description | In this review, we discuss emerging technologies for drug discovery, which yields novel molecular scaffolds based on natural product-inspired non-traditional peptides expressed using the translation machinery. Unlike natural products, these technologies allow for constructing mRNA-encoding libraries of macrocyclic peptides containing non-canonical sidechains and N-methyl-modified backbones. The complexity of sequence space in such libraries reaches as high as a trillion (>1012), affording initial hits of high affinity ligands against protein targets. Although this article comprehensively covers several related technologies, we discuss in greater detail the technical development and advantages of the Random non-standard Peptide Integration Discovery (RaPID) system, including the recent identification of inhibitors against various therapeutic targets. |
| first_indexed | 2024-12-11T04:38:35Z |
| format | Article |
| id | doaj.art-0c593565c6754ce9a71f51c96c0a90a8 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-11T04:38:35Z |
| publishDate | 2013-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-0c593565c6754ce9a71f51c96c0a90a82022-12-22T01:20:41ZengMDPI AGMolecules1420-30492013-03-011833502352810.3390/molecules18033502Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic PeptidesHiroaki SugaToby PassiouraKenichiro ItoIn this review, we discuss emerging technologies for drug discovery, which yields novel molecular scaffolds based on natural product-inspired non-traditional peptides expressed using the translation machinery. Unlike natural products, these technologies allow for constructing mRNA-encoding libraries of macrocyclic peptides containing non-canonical sidechains and N-methyl-modified backbones. The complexity of sequence space in such libraries reaches as high as a trillion (>1012), affording initial hits of high affinity ligands against protein targets. Although this article comprehensively covers several related technologies, we discuss in greater detail the technical development and advantages of the Random non-standard Peptide Integration Discovery (RaPID) system, including the recent identification of inhibitors against various therapeutic targets.http://www.mdpi.com/1420-3049/18/3/3502non-standard macrocyclic peptidesnon-canonical amino acidsflexizymeRandom non-standard Peptide Integration Discovery (RaPID) systempeptide inhibitors |
| spellingShingle | Hiroaki Suga Toby Passioura Kenichiro Ito Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides Molecules non-standard macrocyclic peptides non-canonical amino acids flexizyme Random non-standard Peptide Integration Discovery (RaPID) system peptide inhibitors |
| title | Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides |
| title_full | Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides |
| title_fullStr | Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides |
| title_full_unstemmed | Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides |
| title_short | Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides |
| title_sort | technologies for the synthesis of mrna encoding libraries and discovery of bioactive natural product inspired non traditional macrocyclic peptides |
| topic | non-standard macrocyclic peptides non-canonical amino acids flexizyme Random non-standard Peptide Integration Discovery (RaPID) system peptide inhibitors |
| url | http://www.mdpi.com/1420-3049/18/3/3502 |
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