Teicoplanin: an alternative drug for the treatment of COVID-19?

Baron, Sophie Alexandra; Devaux, Christian; Colson, Philippe; Raoult, Didier; Rolain, Jean‐Marc

doi:10.1016/j.ijantimicag.2020.105944

Cited by 249 publications

(204 citation statements)

References 9 publications

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“…We also observed that the HR2-derived inhibitors were more effective in inhibiting the S protein-mediated cell fusion than their inhibitions on pseudoviruses, implying that SARS-CoV-2 might also adopt the endosome entry pathway. Indeed, it was recently found that cathepsin L is required for the cell entry of SARS-CoV-2 and teicoplanin, a glycopeptide antibiotic, can specifically inhibit the entry (55, 56).…”

Section: Discussionmentioning

confidence: 99%

Design of potent membrane fusion inhibitors against SARS-CoV-2, an emerging coronavirus with high fusogenic activity

Zhu

Huang

et al. 2020

Preprint

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AbstractThe coronavirus disease COVID-19, caused by emerging SARS-CoV-2, has posed serious threats to global public health, economic and social stabilities, calling for the prompt development of therapeutics and prophylactics. In this study, we firstly verified that SARS-CoV-2 uses human ACE2 as a cell receptor and its spike (S) protein mediates high membrane fusion activity. Comparing to that of SARS-CoV, the heptad repeat 1 (HR1) sequence in the S2 fusion protein of SARS-CoV-2 possesses markedly increased α-helicity and thermostability, as well as a higher binding affinity with its corresponding heptad repeat 2 (HR1) site. Then, we designed a HR2 sequence-based lipopeptide fusion inhibitor, termed IPB02, which showed highly poent activities in inibibiting the SARS-CoV-2 S protein-mediated cell-cell fusion and pseudovirus infection. IPB02 also inhibited the SARS-CoV pseudovirus efficiently. Moreover, the strcuture and activity relationship (SAR) of IPB02 were characterzized with a panel of truncated lipopeptides, revealing the amino acid motifs critical for its binding and antiviral capacities. Therefore, the presented results have provided important information for understanding the entry pathway of SARS-CoV-2 and the design of antivirals that target the membrane fusion step.

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Section: Discussionmentioning

confidence: 99%

Design of potent membrane fusion inhibitors against SARS-CoV-2, an emerging coronavirus with high fusogenic activity

Zhu

Huang

et al. 2020

Preprint

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“…The design of enzyme inhibitors as therapeutic platforms against CoV require the control of multiple pharmacologic features beyond the interaction and ACE-2-and furin-targeting drugs (Baron et al, 2020;Kong et al, 2020). A number of these pharmacologic characteristics show their molecular underpinning in chemical pathways within the biological systems.…”

Section: Enzyme Inhibitors As Therapeutic Platformsmentioning

confidence: 99%

A review on the cleavage priming of the spike protein on coronavirus by angiotensin-converting enzyme-2 and furin

Hasan

Paray

Hussain³

et al. 2020

Journal of Biomolecular Structure and Dynamics

259

233

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The widespread antigenic changes lead to the emergence of a new type of coronavirus (CoV) called as severe acute respiratory syndrome (SARS)-CoV-2 that is immunologically different from the previous circulating species. Angiotensin-converting enzyme-2 (ACE-2) is one of the most important receptors on the cell membrane of the host cells (HCs) which its interaction with spike protein (SP) with a furincleavage site results in the SARS-CoV-2 invasion. Hence, in this review, we presented an overview on the interaction of ACE-2 and furin with SP. As several kinds of CoVs, from various genera, have at their S1/S2 binding site a preserved site, we further surveyed the role of furin cleavage site (FCS) on the life cycle of the CoV. Furthermore, we discussed that the small molecular inhibitors can limit the interaction of ACE-2 and furin with SP and can be used as potential therapeutic platforms to combat the spreading CoV epidemic. Finally, some ongoing challenges and future prospects for the development of potential drugs to promote targeting specific activities of the CoV were reviewed. In conclusion, this review may pave the way for providing useful information about different compounds involved in improving the effectiveness of CoV vaccine or drugs with minimum toxicity against human health. ARTICLE HISTORY

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“…This activity is conserved on the SARS-CoV-2, thus placing teicoplanin as a potential treatment for patients with this virus. 46 Recently, tocilizumab, also known as atlizumab, prescribed for two patients with COVID-19 infection in Iran and has shown promising results. This drug is an immunosuppressive humanized monoclonal antibody against the interleukin-6 receptor (IL-6R) and mainly used for the treatment of rheumatoid arthritis (RA) and IL-6 is a cytokine that plays an important role in immune response.…”

Section: Treatment and Preventionmentioning

confidence: 99%

Immune responses and pathogenesis of SARS‐CoV‐2 during an outbreak in Iran: Comparison with SARS and MERS

Rokni

Ghasemi

Tavakoli

2020

Reviews in Medical Virology

210

216

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SummaryThe beginning of 2020 has seen the emergence of COVID‐19, an outbreak caused by a novel coronavirus, SARS‐CoV‐2, an important pathogen for humans. There is an urgent need to better understand this new virus and to develop ways to control its spread. In Iran, the first case of the COVID‐19 was reported after spread from China and other countries. Fever, cough, and fatigue were the most common symptoms of this virus. In worldwide, the incubation period of COVID‐19 was 3 to 7 days and approximately 80% of infections are mild or asymptomatic, 15% are severe, requiring oxygen, and 5% are critical infections, requiring ventilation. To mount an antiviral response, the innate immune system recognizes molecular structures that are produced by the invasion of the virus. COVID‐19 infection induces IgG antibodies against N protein that can be detected by serum as early as day 4 after the onset of disease and with most patients seroconverting by day 14. Laboratory evidence of clinical patients showed that a specific T‐cell response against SARS‐CoV‐2 is important for the recognition and killing of infected cells, particularly in the lungs of infected individuals. At present, there is no specific antiviral therapy for COVID‐19 and the main treatments are supportive. In this review, we investigated the innate and acquired immune responses in patients who recovered from COVID‐19, which could inform the design of prophylactic vaccines and immunotherapy for the future.

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Teicoplanin: an alternative drug for the treatment of COVID-19?

Cited by 249 publications

References 9 publications

Design of potent membrane fusion inhibitors against SARS-CoV-2, an emerging coronavirus with high fusogenic activity

Design of potent membrane fusion inhibitors against SARS-CoV-2, an emerging coronavirus with high fusogenic activity

A review on the cleavage priming of the spike protein on coronavirus by angiotensin-converting enzyme-2 and furin

Immune responses and pathogenesis of SARS‐CoV‐2 during an outbreak in Iran: Comparison with SARS and MERS

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