Teicoplanin derivatives block spike protein mediated viral entry as pan-SARS-CoV-2 inhibitors
Copyright © 2023. Published by Elsevier Masson SAS..
The rapid emergence of highly transmissible SARS-CoV-2 variants poses serious threat to the efficacy of vaccines and neutralizing antibodies. Thus, there is an urgent need to develop new and effective inhibitors against SARS-CoV-2 and future outbreaks. Here, we have identified a series of glycopeptide antibiotics teicoplanin derivatives that bind to the SARS-CoV-2 spike (S) protein, interrupt its interaction with ACE2 receptor and selectively inhibit viral entry mediated by S protein. Computation modeling predicts that these compounds interact with the residues in the receptor binding domain. More importantly, these teicoplanin derivatives inhibit the entry of both pseudotyped SARS-CoV-2 Delta and Omicron variants. Our study demonstrates the feasibility of developing small molecule entry inhibitors by targeting the interaction of viral S protein and ACE2. Together, considering the proven safety and pharmacokinetics of teicoplanin as a glycopeptide antibiotic, the teicoplanin derivatives hold great promise of being repurposed as pan-SARS-CoV-2 inhibitors.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2023 |
|---|---|
| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:158 |
|---|---|
| Enthalten in: |
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie - 158(2023) vom: 09. Feb., Seite 114213 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Ma, Ling [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 15.03.2023 Date Revised 15.03.2023 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1016/j.biopha.2023.114213 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM354220195 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM354220195 | ||
| 003 | DE-627 | ||
| 005 | 20231226061739.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231226s2023 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1016/j.biopha.2023.114213 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1180.xml |
| 035 | |a (DE-627)NLM354220195 | ||
| 035 | |a (NLM)36916436 | ||
| 035 | |a (PII)S0753-3322(23)00001-X | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Ma, Ling |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Teicoplanin derivatives block spike protein mediated viral entry as pan-SARS-CoV-2 inhibitors |
| 264 | 1 | |c 2023 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 15.03.2023 | ||
| 500 | |a Date Revised 15.03.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2023. Published by Elsevier Masson SAS. | ||
| 520 | |a The rapid emergence of highly transmissible SARS-CoV-2 variants poses serious threat to the efficacy of vaccines and neutralizing antibodies. Thus, there is an urgent need to develop new and effective inhibitors against SARS-CoV-2 and future outbreaks. Here, we have identified a series of glycopeptide antibiotics teicoplanin derivatives that bind to the SARS-CoV-2 spike (S) protein, interrupt its interaction with ACE2 receptor and selectively inhibit viral entry mediated by S protein. Computation modeling predicts that these compounds interact with the residues in the receptor binding domain. More importantly, these teicoplanin derivatives inhibit the entry of both pseudotyped SARS-CoV-2 Delta and Omicron variants. Our study demonstrates the feasibility of developing small molecule entry inhibitors by targeting the interaction of viral S protein and ACE2. Together, considering the proven safety and pharmacokinetics of teicoplanin as a glycopeptide antibiotic, the teicoplanin derivatives hold great promise of being repurposed as pan-SARS-CoV-2 inhibitors | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Angiotensin converting enzyme 2 | |
| 650 | 4 | |a Entry inhibitor | |
| 650 | 4 | |a SARS-CoV-2 | |
| 650 | 4 | |a Spike protein | |
| 650 | 4 | |a Teicoplanin | |
| 650 | 7 | |a Teicoplanin |2 NLM | |
| 650 | 7 | |a 61036-62-2 |2 NLM | |
| 650 | 7 | |a Angiotensin-Converting Enzyme 2 |2 NLM | |
| 650 | 7 | |a EC 3.4.17.23 |2 NLM | |
| 650 | 7 | |a spike protein, SARS-CoV-2 |2 NLM | |
| 650 | 7 | |a Spike Glycoprotein, Coronavirus |2 NLM | |
| 650 | 7 | |a Anti-Bacterial Agents |2 NLM | |
| 700 | 1 | |a Li, Yali |e verfasserin |4 aut | |
| 700 | 1 | |a Shi, Ting |e verfasserin |4 aut | |
| 700 | 1 | |a Zhu, Zhiling |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Jianyuan |e verfasserin |4 aut | |
| 700 | 1 | |a Xie, Yongli |e verfasserin |4 aut | |
| 700 | 1 | |a Wen, Jiajia |e verfasserin |4 aut | |
| 700 | 1 | |a Guo, Saisai |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Jing |e verfasserin |4 aut | |
| 700 | 1 | |a Ding, Jiwei |e verfasserin |4 aut | |
| 700 | 1 | |a Liang, Chen |e verfasserin |4 aut | |
| 700 | 1 | |a Shan, Guangzhi |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Quanjie |e verfasserin |4 aut | |
| 700 | 1 | |a Ge, Mei |e verfasserin |4 aut | |
| 700 | 1 | |a Cen, Shan |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie |d 1984 |g 158(2023) vom: 09. Feb., Seite 114213 |w (DE-627)NLM012645591 |x 1950-6007 |7 nnns |
| 773 | 1 | 8 | |g volume:158 |g year:2023 |g day:09 |g month:02 |g pages:114213 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1016/j.biopha.2023.114213 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 158 |j 2023 |b 09 |c 02 |h 114213 | ||