Further structural optimization and SAR study of sungsanpin derivatives as cell-invasion inhibitors
Copyright © 2024 Elsevier Ltd. All rights reserved..
Metastasis is one of the major causes of death in patients with cancer, and cell invasion plays a fundamental part in this process. Because of the absence of efficacious treatments, caring for these patients is challenging. Recently, we optimized the structure of the naturally occurring lasso peptide sungsanpin. We identified two peptides, octapeptide S3 and cyclic peptide S4, which inhibited invasion into A549 cells effectively. We undertook an alanine scan of S3 to explore the structure-activity relationship. The linear octapeptide S3-4 and cyclic peptide S4-1 exhibited improved inhibition of invasion into A549 cells. We modified S3-4 to obtain S3-4K, which displayed much higher inhibitory activity against invasion into A549 cells than S3-4. Of all peptides tested, S4-1 upregulated significantly mRNA of tissue inhibitor matrix metalloproteinase TIMP-1 and TIMP-2.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:99 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 99(2024) vom: 01. Feb., Seite 129627 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chen, Shuai [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 06.02.2024 Date Revised 06.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2024.129627 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Copyright © 2024 Elsevier Ltd. All rights reserved. | ||
| 520 | |a Metastasis is one of the major causes of death in patients with cancer, and cell invasion plays a fundamental part in this process. Because of the absence of efficacious treatments, caring for these patients is challenging. Recently, we optimized the structure of the naturally occurring lasso peptide sungsanpin. We identified two peptides, octapeptide S3 and cyclic peptide S4, which inhibited invasion into A549 cells effectively. We undertook an alanine scan of S3 to explore the structure-activity relationship. The linear octapeptide S3-4 and cyclic peptide S4-1 exhibited improved inhibition of invasion into A549 cells. We modified S3-4 to obtain S3-4K, which displayed much higher inhibitory activity against invasion into A549 cells than S3-4. Of all peptides tested, S4-1 upregulated significantly mRNA of tissue inhibitor matrix metalloproteinase TIMP-1 and TIMP-2 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Cancer invasion | |
| 650 | 4 | |a MMP | |
| 650 | 4 | |a Peptide drug design | |
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| 700 | 1 | |a Zou, Jihua |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Zhou |e verfasserin |4 aut | |
| 700 | 1 | |a Gai, Conghao |e verfasserin |4 aut | |
| 700 | 1 | |a Chai, Xiaoyun |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Qingjie |e verfasserin |4 aut | |
| 700 | 1 | |a Zou, Yan |e verfasserin |4 aut | |
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