Benzyl stapled modification and anticancer activity of antimicrobial peptide A4K14-Citropin 1.1
Copyright © 2023 Elsevier Ltd. All rights reserved..
A4K14-Citropin 1.1 (GLFAVIKKVASVIKGL-NH2) is a derived antimicrobial peptide (AMP) with a more stable α-helical structure at the C-terminal compared to prototype Citropin 1.1 which was obtained from glandular skin secretions of Australian freetail lizards. In a previous report, A4K14-Citropin 1.1 has been considered as an anti-cancer lead compound. However, linear peptides are difficult to maintain stable secondary structure, resulted in poor pharmacokinetic properties. In this study, we designed and synthesized a series of benzyl-stapled derivatives of A4K14-Citropin 1.1. And their physical and chemical properties, as well as biological activity, were both explored. The result showed that AC-CCSP-2-o and AC-CCSP-3-o exhibited a higher degree of helicity and greater anti-cancer activity compared with the prototype peptide. Besides, there was no significant difference in the hemolytic effect between the stapled peptides and the prototype peptide. AC-CCSP-2-o and AC-CCSP-3-o could serve as promising anti-cancer lead compounds for the novel anti-cancer drug development.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:96 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 96(2023) vom: 15. Nov., Seite 129499 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Shen, Huaxing [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 20.11.2023 Date Revised 20.11.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2023.129499 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM362985847 |
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| 245 | 1 | 0 | |a Benzyl stapled modification and anticancer activity of antimicrobial peptide A4K14-Citropin 1.1 |
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| 500 | |a Date Revised 20.11.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2023 Elsevier Ltd. All rights reserved. | ||
| 520 | |a A4K14-Citropin 1.1 (GLFAVIKKVASVIKGL-NH2) is a derived antimicrobial peptide (AMP) with a more stable α-helical structure at the C-terminal compared to prototype Citropin 1.1 which was obtained from glandular skin secretions of Australian freetail lizards. In a previous report, A4K14-Citropin 1.1 has been considered as an anti-cancer lead compound. However, linear peptides are difficult to maintain stable secondary structure, resulted in poor pharmacokinetic properties. In this study, we designed and synthesized a series of benzyl-stapled derivatives of A4K14-Citropin 1.1. And their physical and chemical properties, as well as biological activity, were both explored. The result showed that AC-CCSP-2-o and AC-CCSP-3-o exhibited a higher degree of helicity and greater anti-cancer activity compared with the prototype peptide. Besides, there was no significant difference in the hemolytic effect between the stapled peptides and the prototype peptide. AC-CCSP-2-o and AC-CCSP-3-o could serve as promising anti-cancer lead compounds for the novel anti-cancer drug development | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a A4K14-Citropin 1.1 | |
| 650 | 4 | |a AMP | |
| 650 | 4 | |a Anti-cancer activity | |
| 650 | 4 | |a Antimicrobial peptide | |
| 650 | 4 | |a Thiol-halogen click chemistry | |
| 650 | 7 | |a Antimicrobial Cationic Peptides |2 NLM | |
| 650 | 7 | |a Antimicrobial Peptides |2 NLM | |
| 650 | 7 | |a Amphibian Proteins |2 NLM | |
| 700 | 1 | |a Zhang, Nan |e verfasserin |4 aut | |
| 700 | 1 | |a Kong, Xianglong |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Nan |e verfasserin |4 aut | |
| 700 | 1 | |a Hu, Hong-Gang |e verfasserin |4 aut | |
| 700 | 1 | |a Cong, Wei |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Chao |e verfasserin |4 aut | |
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