Peptide Stapling Applied to Antimicrobial Peptides
Antimicrobial peptides (AMPs) are considered a promising therapeutic approach against multi-drug resistant microorganisms. Besides their advantages, there are limitations to be overcome so that these molecules can become market competitive. One of the biggest limitations is proteolytic susceptibilit...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-09-01
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| Series: | Antibiotics |
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| Online Access: | https://www.mdpi.com/2079-6382/12/9/1400 |
| _version_ | 1827727515137867776 |
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| author | Ana Laura Pereira Lourenço Thuanny Borba Rios Állan Pires da Silva Octávio Luiz Franco Marcelo Henrique Soller Ramada |
| author_facet | Ana Laura Pereira Lourenço Thuanny Borba Rios Állan Pires da Silva Octávio Luiz Franco Marcelo Henrique Soller Ramada |
| author_sort | Ana Laura Pereira Lourenço |
| collection | DOAJ |
| description | Antimicrobial peptides (AMPs) are considered a promising therapeutic approach against multi-drug resistant microorganisms. Besides their advantages, there are limitations to be overcome so that these molecules can become market competitive. One of the biggest limitations is proteolytic susceptibility, which could be overcome by structural modifications such as cyclization, especially for helix-constraining strategies. Over the years, many helix stabilization techniques have arisen, such as lactam-bridging, triazole-based, N-alkylation and all-hydrocarbon stapling. All-hydrocarbon stapling takes advantage of modified amino acid residues and olefinic cross-linking to constrain peptide helices. Despite being a well-established strategy and presenting efficient stability results, there are different limitations especially related to toxicity. In this review, recent studies on stapled AMPs for antimicrobial usage are explored with the aim of understanding the future of these molecules as putative antimicrobial agents. |
| first_indexed | 2024-03-10T23:06:32Z |
| format | Article |
| id | doaj.art-7b4c711d77044fedb051805b675b6210 |
| institution | Directory Open Access Journal |
| issn | 2079-6382 |
| language | English |
| last_indexed | 2024-03-10T23:06:32Z |
| publishDate | 2023-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antibiotics |
| spelling | doaj.art-7b4c711d77044fedb051805b675b62102023-11-19T09:17:14ZengMDPI AGAntibiotics2079-63822023-09-01129140010.3390/antibiotics12091400Peptide Stapling Applied to Antimicrobial PeptidesAna Laura Pereira Lourenço0Thuanny Borba Rios1Állan Pires da Silva2Octávio Luiz Franco3Marcelo Henrique Soller Ramada4Programa de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília, Brasília 71966-700, BrazilPrograma de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília, Brasília 71966-700, BrazilPrograma de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília, Brasília 71966-700, BrazilPrograma de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília, Brasília 71966-700, BrazilPrograma de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília, Brasília 71966-700, BrazilAntimicrobial peptides (AMPs) are considered a promising therapeutic approach against multi-drug resistant microorganisms. Besides their advantages, there are limitations to be overcome so that these molecules can become market competitive. One of the biggest limitations is proteolytic susceptibility, which could be overcome by structural modifications such as cyclization, especially for helix-constraining strategies. Over the years, many helix stabilization techniques have arisen, such as lactam-bridging, triazole-based, N-alkylation and all-hydrocarbon stapling. All-hydrocarbon stapling takes advantage of modified amino acid residues and olefinic cross-linking to constrain peptide helices. Despite being a well-established strategy and presenting efficient stability results, there are different limitations especially related to toxicity. In this review, recent studies on stapled AMPs for antimicrobial usage are explored with the aim of understanding the future of these molecules as putative antimicrobial agents.https://www.mdpi.com/2079-6382/12/9/1400antimicrobial peptidesstaplingall-hydrocarbon staplingcyclization |
| spellingShingle | Ana Laura Pereira Lourenço Thuanny Borba Rios Állan Pires da Silva Octávio Luiz Franco Marcelo Henrique Soller Ramada Peptide Stapling Applied to Antimicrobial Peptides Antibiotics antimicrobial peptides stapling all-hydrocarbon stapling cyclization |
| title | Peptide Stapling Applied to Antimicrobial Peptides |
| title_full | Peptide Stapling Applied to Antimicrobial Peptides |
| title_fullStr | Peptide Stapling Applied to Antimicrobial Peptides |
| title_full_unstemmed | Peptide Stapling Applied to Antimicrobial Peptides |
| title_short | Peptide Stapling Applied to Antimicrobial Peptides |
| title_sort | peptide stapling applied to antimicrobial peptides |
| topic | antimicrobial peptides stapling all-hydrocarbon stapling cyclization |
| url | https://www.mdpi.com/2079-6382/12/9/1400 |
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