Recent advances in small-molecular therapeutics for COVID-19

Article Pharmacology & Pharmacy

Very low levels of remdesivir resistance in SARS-COV-2 genomes after 18 months of massive usage during the COVID19 pandemic: A GISAID exploratory analysis

Daniele Focosi et al.

Summary: Despite massive usage, the global level of remdesivir resistance is very low during the COVID-19 pandemic.

ANTIVIRAL RESEARCH (2022)

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Article Biochemistry & Molecular Biology

Suramin, penciclovir, and anidulafungin exhibit potential in the treatment of COVID-19 via binding to nsp12 of SARS-CoV-2

Sanjay Kumar Dey et al.

Summary: Research suggests that certain drugs may have potential therapeutic effects against COVID-19 by interacting significantly with viral enzymes, which could be used as monotherapy or in combination with Remdesivir.

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS (2022)

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Article Medicine, General & Internal

Oral Nirmatrelvir for High-Risk, Nonhospitalized Adults with Covid-19

Jennifer Hammond et al.

Summary: In high-risk, unvaccinated adults, treatment of Covid-19 with nirmatrelvir plus ritonavir can significantly reduce the risk of hospitalization and death, with good safety profile.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

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Article Medicine, General & Internal

Early Remdesivir to Prevent Progression to Severe Covid-19 in Outpatients

R. L. Gottlieb et al.

Summary: In symptomatic, nonhospitalized high-risk Covid-19 patients, a 3-day course of remdesivir significantly reduced the risk of hospitalization or death compared to placebo, with acceptable safety profile.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

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Article Chemistry, Multidisciplinary

Newly synthesized series of oxoindole-oxadiazole conjugates as potential anti-SARS-CoV-2 agents: in silico and in vitro studies

Rana M. El-Masry et al.

Summary: In this study, a series of anti-SARS-CoV-2 agents were designed and synthesized, and their binding affinities and virus-inhibitory concentrations were evaluated. Compounds IVe and IVg showed high activity and have the potential to be developed as broad-spectrum anti-SARS-CoV-2 agents.

NEW JOURNAL OF CHEMISTRY (2022)

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Review Endocrinology & Metabolism

An updated practical guideline on use of molnupiravir and comparison with agents having emergency use authorization for treatment of COVID-19

Awadhesh Kumar Singh et al.

Summary: Molnupiravir is an oral antiviral drug that has received emergency use authorization in the USA, UK, and India. Recent studies have shown that it can significantly reduce the risk of hospitalization or death in non-hospitalized COVID-19 patients. Molnupiravir is comparatively cheaper than other agents and can be an effective option for treating COVID-19, but it needs to be used within 5 days of symptom onset.

DIABETES & METABOLIC SYNDROME-CLINICAL RESEARCH & REVIEWS (2022)

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Article Chemistry, Multidisciplinary

Safety, tolerability, and pharmacokinetics of VV116, an oral nucleoside analog against SARS-CoV-2, in Chinese healthy subjects

Hong-jie Qian et al.

Summary: VV116, an oral drug candidate against SARS-CoV-2, showed satisfactory safety and tolerability in healthy subjects, with no significant impact from food intake. These findings support further investigation of VV116 in patients with COVID-19.

ACTA PHARMACOLOGICA SINICA (2022)

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Review Biochemistry & Molecular Biology

Potential Resistance of SARS-CoV-2 Main Protease (Mpro) against Protease Inhibitors: Lessons Learned from HIV-1 Protease

Janos Andras Motyan et al.

Summary: COVID-19 is a devastating pandemic caused by SARS-CoV-2. The lack of effective antiviral drugs has led to global health crises. Pfizer's newly approved nirmatrelvir has shown promise as an inhibitor of the viral main protease, offering hope for both therapeutic and prophylactic use against the infection. However, the high mutation rates of RNA viruses highlight the importance of considering lessons learned from previous pandemics to avoid the emergence of resistance mutations in long-term use of novel inhibitors.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

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News Item Multidisciplinary Sciences

Are COVID surges becoming more predictable? New Omicron variants offer a hint

Ewen Callaway

NATURE (2022)

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News Item Multidisciplinary Sciences

A DELUGE OF NEW DRUGS FOR COVID

Heidi Ledford

Summary: Two years into the pandemic, the development of COVID-19 therapeutics is progressing well, introducing innovative treatments and discovering new applications for existing drugs.

NATURE (2022)

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Article Immunology

Paxlovid (Nirmatelvir/Ritonavir) and Tacrolimus Drug-Drug Interaction in a Kidney Transplant Patient with SARS-2-CoV infection: A Case Report

Marios Prikis et al.

Summary: The COVID-19 pandemic has impacted communities and health systems significantly, and new antiviral medications have not been thoroughly tested. Drug interactions may affect the treatment outcomes of organ transplant recipients, emphasizing the importance of monitoring for adverse effects.

TRANSPLANTATION PROCEEDINGS (2022)

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Review Chemistry, Medicinal

A Systematic Review of the Global Intervention for SARS-CoV-2 Combating: From Drugs Repurposing to Molnupiravir Approval

Nada A. Ashour et al.

Summary: This article provides a comprehensive review of drug repurposing for COVID-19 and the latest available oral anti-SARS-CoV-2 medications, discussing clinical trials, combination therapies, novel methods, and future prospects.

DRUG DESIGN DEVELOPMENT AND THERAPY (2022)

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Review Pharmacology & Pharmacy

Recent advances in developing small-molecule inhibitors against SARS-CoV-2

Rong Xiang et al.

Summary: The COVID-19 pandemic has caused chaos worldwide, with vaccines in distribution but treatment methods lagging behind. Researchers are working hard to understand the virus and develop effective treatments.

ACTA PHARMACEUTICA SINICA B (2022)

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Review Immunology

Molnupiravir and Its Antiviral Activity Against COVID-19

Lili Tian et al.

Summary: Molnupiravir is a broad-spectrum antiviral drug with the potential to treat and prevent various coronaviruses, including SARS-CoV-2. Clinical trials have shown its beneficial effects and favorable safety profile for mild to moderate COVID-19 patients. Molnupiravir has the potential to be a therapeutic candidate against COVID-19.

FRONTIERS IN IMMUNOLOGY (2022)

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Article Medicine, General & Internal

Favipiravir, camostat, and ciclesonide combination therapy in patients with moderate COVID-19 pneumonia with/without oxygen therapy: An open- label, single-center phase 3 randomized clinical trial

Jiro Terada et al.

Summary: This study evaluated the effectiveness of combination therapy with favipiravir, camostat, and ciclesonide in patients with moderate COVID-19 pneumonia. The combination therapy was found to reduce the length of hospital stay without safety concerns. However, the study had limitations due to the lack of a hard clinical primary outcome.

ECLINICALMEDICINE (2022)

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Article Critical Care Medicine

Use of Ivermectin Is Associated With Lower Mortality in Hospitalized Patients With Coronavirus Disease 2019 The Ivermectin in COVID Nineteen Study

Juliana Cepelowicz Rajter et al.

Summary: Ivermectin treatment was associated with lower mortality in COVID-19 patients, especially those with severe pulmonary involvement, suggesting its potential effectiveness in reducing mortality in hospitalized COVID-19 patients. Randomized controlled trials are needed to confirm these findings.

CHEST (2021)

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Article Pharmacology & Pharmacy

Clinical Outcomes and Plasma Concentrations of Baloxavir Marboxil and Favipiravir in COVID-19 Patients: An Exploratory Randomized, Controlled Trial

Yan Lou et al.

Summary: Effective antiviral drugs for COVID-19 are still lacking and this study aimed to evaluate the clinical outcomes and plasma concentrations of baloxavir acid and favipiravir in COVID-19 patients. In vitro evaluation showed that baloxavir acid exhibited antiviral activity, while favipiravir did not demonstrate significant antiviral activity. However, the addition of either baloxavir marboxil or favipiravir under the trial dosages did not show clear benefits compared to standard treatment.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2021)

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Review Microbiology

Characteristics of SARS-CoV-2 and COVID-19

Ben Hu et al.

Summary: This review summarizes the research progress on SARS-CoV-2 and COVID-19, including virology characteristics, pathogenesis, and recent advances in treatment methods. Furthermore, it discusses in detail the potential wildlife hosts and zoonotic origin of this emerging virus.

NATURE REVIEWS MICROBIOLOGY (2021)

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Article Chemistry, Multidisciplinary

Molecular Simulations suggest Vitamins, Retinoids and Steroids as Ligands of the Free Fatty Acid Pocket of the SARS-CoV-2 Spike Protein**

Deborah K. Shoemark et al.

Summary: The study found that linoleate and dexamethasone can stabilize the conformation of the SARS-CoV-2 spike protein, reducing its interaction with ACE2, while cholesterol may expose the receptor-binding domain. Furthermore, steroids, retinoids, and vitamins were identified as potential ligands that may stabilize the closed conformation.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Letter Cell Biology

Design and development of an oral remdesivir derivative VV116 against SARS-CoV-2

Yuanchao Xie et al.

CELL RESEARCH (2021)

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Article Respiratory System

Early use of nitazoxanide in mild COVID-19 disease: randomised, placebo-controlled trial

Patricia R. M. Rocco et al.

Summary: In patients with mild COVID-19, there was no difference in symptom resolution between nitazoxanide and placebo groups after 5 days of treatment, but early nitazoxanide therapy significantly reduced viral load.

EUROPEAN RESPIRATORY JOURNAL (2021)

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Article Medicine, General & Internal

Repurposed Antiviral Drugs for Covid-19-Interim WHO Solidarity Trial Results

Summary: The authors of the study reported the interim results of using four repurposed antiviral drugs (remdesivir, hydroxychloroquine, lopinavir, and interferon beta-1a) in hospitalized COVID-19 patients. The study showed that these drug regimens had little or no effect on overall mortality, initiation of ventilation, and duration of hospital stay.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

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Article Medicine, General & Internal

Baricitinib plus Remdesivir for Hospitalized Adults with Covid-19

A. C. Kalil et al.

Summary: Combination treatment with baricitinib plus remdesivir was superior to remdesivir alone in reducing recovery time and accelerating improvement in clinical status among patients with Covid-19, notably among those receiving high-flow oxygen or noninvasive ventilation. The combination was associated with fewer serious adverse events.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

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Article Multidisciplinary Sciences

Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2

Yuanyuan Qiao et al.

Summary: Research has shown that androgens regulate the expression of ACE2, TMPRSS2, and AR in lung epithelial cells, affecting the risk of COVID-19 infection in males over 70 years old. The use of AR or BET antagonists can inhibit SARS-CoV-2 infection, providing support for further investigation into transcriptional inhibition for the treatment or prevention of COVID-19.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

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Article Chemistry, Medicinal

The SARS-CoV-2 Cytopathic Effect Is Blocked by Lysosome Alkalizing Small Molecules

Kirill Gorshkov et al.

Summary: Research has found that certain compounds can block the cytopathic effects of SARS-CoV-2 in cells by affecting lysosome functioning, autophagy, and reducing viral titers. This suggests the lysosome may play a role in the lifecycle of SARS-CoV-2, making inhibitors of lysosomal function a potential target for combating infections and improving treatment outcomes for COVID-19.

ACS INFECTIOUS DISEASES (2021)

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Article Multidisciplinary Sciences

High-throughput rational design of the remdesivir binding site in the RdRp of SARS-CoV-2: implications for potential resistance

Aditya K. Padhi et al.

Summary: With the use of mutational mapping, it was predicted that only a few mutations in the nsp12 subunit of RdRp are needed for SARS-CoV-2 to develop resistance to remdesivir. Certain mutations resulted in decreased binding affinity to remdesivir, indicating drug resistance. Identifying potential hotspot residues prone to mutation improves our understanding of SARS-CoV-2 drug resistance and COVID-19 pathogenesis.

ISCIENCE (2021)

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Article Biology

Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents

Vicky Mody et al.

Summary: The study identified potential drugs that target the pivotal protease 3-chymotrypsin like protease (3CLpro) for SARS-CoV-2 replication. Some of these drugs showed inhibitory effects on the enzyme activity, suggesting they could be useful in inhibiting SARS-CoV-2 replication.

COMMUNICATIONS BIOLOGY (2021)

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Article Microbiology

Human Safety, Tolerability, and Pharmacokinetics of Molnupiravir, a Novel Broad-Spectrum Oral Antiviral Agent with Activity against SARS-CoV-2

Wendy P. Painter et al.

Summary: Molnupiravir showed rapid appearance and dose-proportional increase in plasma, with good tolerability in healthy volunteers. The study evaluated single and multiple doses of molnupiravir and the impact of food on pharmacokinetics in subjects, showing no accumulation following multiple doses and a decrease in absorption rate when administered with food, but no decrease in overall exposure.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2021)

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Article Microbiology

Kinetic Characterization and Inhibitor Screening for the Proteases Leading to Identification of Drugs against SARS-CoV-2

Chih-Jung Kuo et al.

Summary: This study established assay platforms for 3CL(pro) and PLpro, screening FDA-approved drugs as potential inhibitors for SARS-CoV-2, providing candidate drugs for the prevention and treatment of COVID-19.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2021)

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Article Microbiology

AT-527, a Double Prodrug of a Guanosine Nucleotide Analog, Is a Potent Inhibitor of SARS-CoV-2 In Vitro and a Promising Oral Antiviral for Treatment of COVID-19

Steven S. Good et al.

Summary: AT-527, an oral antiviral drug, has potent activity against various coronaviruses, including SARS-CoV-2. In vitro experiments have shown that AT-511 has high efficacy in inhibiting the replication of SARS-CoV-2, with minimal cytotoxicity. Studies suggest that AT-527 may be an effective treatment option for COVID-19.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2021)

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Article Immunology

Safety and efficacy of Favipiravir in moderate to severe SARS-CoV-2 pneumonia

Masoud Solaymani-Dodaran et al.

Summary: The study found that adding Favipiravir to the treatment protocol did not reduce ICU admissions, intubations, or in-hospital mortality compared to the Lopinavir/Ritonavir regimen. There were also no significant differences in time to clinical recovery and length of hospital stay between the two treatment groups.

INTERNATIONAL IMMUNOPHARMACOLOGY (2021)

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Article Infectious Diseases

Efficacy and safety of favipiravir, an oral RNA-dependent RNA polymerase inhibitor, in mild-to-moderate COVID-19: A randomized, comparative, open-label, multicenter, phase 3 clinical trial

Zarir F. Udwadia et al.

Summary: The study aimed to assess the efficacy and safety of favipiravir in adults with mild-to-moderate COVID-19. Results showed a significant improvement in time to clinical cure with favipiravir, although there was no statistically significant difference in viral shedding cessation time.

INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES (2021)

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Article Medicine, General & Internal

Effect of Ivermectin on Time to Resolution of Symptoms Among Adults With Mild COVID-19 A Randomized Clinical Trial

Eduardo Lopez-Medina et al.

Summary: The study found that a 5-day course of ivermectin did not significantly improve the time to resolution of symptoms in adults with mild COVID-19, and does not support its use for treatment of mild COVID-19. Larger trials may be needed to understand the effects of ivermectin on other clinically relevant outcomes.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2021)

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Article Multidisciplinary Sciences

SARS-CoV-2 infection is effectively treated and prevented by EIDD-2801

Angela Wahl et al.

Summary: The study suggests that bats may be the source of coronaviruses that can be directly transmitted to humans. Using the LoM model, efficient replication of SARS-CoV, MERS-CoV, SARS-CoV-2, and two SARS-like bat coronaviruses in human lung tissue was demonstrated. Infection with SARS-CoV-2 predominantly targets human lung epithelial cells and induces a sustained inflammatory response. The broad-spectrum antiviral agent EIDD-2801 significantly inhibits SARS-CoV-2 replication in vivo, showing potential for prevention and treatment of COVID-19.

NATURE (2021)

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Article Medicine, General & Internal

Interleukin-6 Receptor Antagonists in Critically Ill Patients with Covid-19

Anthony C. Gordon et al.

Summary: Interleukin-6 receptor antagonists tocilizumab and sarilumab were found to improve outcomes, including survival, in critically ill patients with Covid-19 receiving organ support in ICUs according to an ongoing international trial. The efficacy of these treatments has been confirmed, with patients benefiting from the therapy.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

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Article Multidisciplinary Sciences

An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

Dafydd R. Owen et al.

Summary: PF-07321332, an orally bioavailable SARS-CoV-2 main protease inhibitor, has been discovered with in vitro pan-human coronavirus antiviral activity and excellent off-target selectivity and in vivo safety profiles. This new drug has shown promise in countering the threat of COVID-19 with its oral activity and safety in clinical trials.

SCIENCE (2021)

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Article Multidisciplinary Sciences

Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A

Kris M. White et al.

Summary: The study revealed that plitidepsin possesses potent antiviral activity against SARS-CoV-2, more effective than the approved drug remdesivir. By inhibiting the eukaryotic translation elongation factor 1A, plitidepsin can significantly reduce viral replication of SARS-CoV-2 in the lungs of mice, making it a promising candidate for COVID-19 treatment.

SCIENCE (2021)

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Article Multidisciplinary Sciences

Intranasal fusion inhibitory lipopeptide prevents direct-contact SARS-CoV-2 transmission in ferrets

Rory D. de Vries et al.

Summary: The lipopeptide fusion inhibitors designed effectively blocked the critical first step of SARS-CoV-2 infection. Daily intranasal administration to ferrets prevented transmission completely, showcasing potential as safe and effective prophylaxis for reducing SARS-CoV-2 transmission.

SCIENCE (2021)

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Article Multidisciplinary Sciences

Structure of papain-like protease from SARS-CoV-2 and its complexes with non-covalent inhibitors

Jerzy Osipiuk et al.

Summary: The study focused on papain-like protease (PLpro) as a potential target for antivirals against SARS-CoV-2, identifying inhibitors and their interactions with the enzyme. The findings demonstrate the potential for developing high-affinity inhibitors through structure-based drug design efforts targeting PLpro.

NATURE COMMUNICATIONS (2021)

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Article Multidisciplinary Sciences

Identification of ebselen and its analogues as potent covalent inhibitors of papain-like protease from SARS-CoV-2

Ewelina Weglarz-Tomczak et al.

Summary: Organoselenium compounds were identified as a novel approach for inhibiting the activity of PL(pro)CoV2, with inhibitors showing potency in the nanomolar range for the first time. Differences between PLpro from SARS and CoV2 were also found, potentially correlating with the diverse dynamics of their replication and disease progression.

SCIENTIFIC REPORTS (2021)

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Article Chemistry, Medicinal

Challenges for Targeting SARS-CoV-2 Proteases as a Therapeutic Strategy for COVID-19

Kas Steuten et al.

Summary: Two proteases produced by the SARS-CoV-2 virus play essential roles in viral replication, but inhibitors may also affect host cells; careful assessment of the selectivity of protease inhibitors is needed during drug development to avoid unnecessary interference with redundant pathways for viral entry.

ACS INFECTIOUS DISEASES (2021)

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Article Medicine, General & Internal

Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity

Markus Hoffmann et al.

Summary: The study demonstrates that Camostat mesylate and its metabolite GBPA can block the spread of SARS-CoV-2 in human lung tissue, and the related protease inhibitor Nafamostat mesylate exhibits enhanced antiviral activity.

EBIOMEDICINE (2021)

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News Item Medicine, General & Internal

Covid-19: Molnupiravir reduces risk of hospital admission or death by 50% in patients at risk, MSD reports

Elisabeth Mahase

BMJ-BRITISH MEDICAL JOURNAL (2021)

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Article Pharmacology & Pharmacy

Genetic conservation of SARS-CoV-2 RNA replication complex in globally circulating isolates and recently emerged variants from humans and minks suggests minimal pre-existing resistance to remdesivir

Ross Martin et al.

Summary: The study reveals low genetic variation in the RNA replication complex of SARS-CoV-2, especially the RNA-dependent RNA polymerase (nsp12), which is the main target of remdesivir. The risk of pre-existing resistance to remdesivir is minimal.

ANTIVIRAL RESEARCH (2021)

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Article Biochemistry & Molecular Biology

SARS-CoV-2 Papain-Like Protease Potential Inhibitors-In Silico Quantitative Assessment

Adam Stasiulewicz et al.

Summary: In this study, 387 potential, selective PLpro inhibitors were identified through computational screening, with 20 best compounds selected based on their IC50 values. These candidates showed potential activity against the protein in the nanomolar range and mostly adopted a similar binding mode to known inhibitors. Six most promising compounds were further proposed for future in vitro evaluation.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

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Article Medicine, General & Internal

The combined treatment of Molnupiravir and Favipiravir results in a potentiation of antiviral efficacy in a SARS-CoV-2 hamster infection model

Rana Abdelnabi et al.

Summary: The combination of Molnupiravir and Favipiravir demonstrated a significant antiviral effect in a Syrian hamster model infected with SARS-CoV-2, reducing infectious virus titers in the lungs and preventing transmission to co-housed untreated sentinels. Mutation frequency in the viral RNA recovered from the lungs of treated animals increased, with a higher frequency of C-to-T mutations observed in the combo treatment group, explaining the pronounced antiviral potency of the combination.

EBIOMEDICINE (2021)

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Article Immunology

β-D-N4-hydroxycytidine Inhibits SARS-CoV-2 Through Lethal Mutagenesis But Is Also Mutagenic To Mammalian Cells

Shuntai Zhou et al.

Summary: Mutagenic ribonucleosides can serve as broad-spectrum antiviral agents, but may pose risks to the host due to their host mutagenic activity in addition to antiviral activity.

JOURNAL OF INFECTIOUS DISEASES (2021)

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Article Multidisciplinary Sciences

Clofazimine broadly inhibits coronaviruses including SARS-CoV-2

Shuofeng Yuan et al.

Summary: The anti-leprosy drug clofazimine has shown inhibitory activity against various coronaviruses, reducing viral loads in the lung and shedding, as well as alleviating inflammation. Combination with remdesivir exhibited antiviral synergy, suggesting potential for treating COVID-19 patients, particularly in resource-limited settings.

NATURE (2021)

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Article Multidisciplinary Sciences

Drugs that inhibit TMEM16 proteins block SARS-CoV-2 spike-induced syncytia

Luca Braga et al.

Summary: COVID-19 patients' lungs contain infected pneumocytes with abnormal morphology and frequent multinucleation, leading to the formation of syncytia driven by the activation of the SARS-CoV-2 spike protein. The antihelminthic drug niclosamide has shown to effectively inhibit cell fusion, potentially providing a new therapeutic approach for COVID-19 disease pathogenesis.

NATURE (2021)

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Article Medicine, General & Internal

Efficacy of the ChAdOx1 nCoV-19 Covid-19 Vaccine against the B.1.351 Variant

S. A. Madhi et al.

Summary: The ChAdOx1 nCoV-19 vaccine did not provide significant protection against mild-to-moderate Covid-19 caused by the B.1.351 variant, with an efficacy of 10.4%. The incidence of serious adverse events was balanced between the vaccine and placebo groups.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

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Review Endocrinology & Metabolism

Molnupiravir in COVID-19: A systematic review of literature

Awadhesh Kumar Singh et al.

Summary: Molnupiravir has shown significant benefits in reducing hospitalization or death in mild COVID-19 cases, making it a potential important tool in combating SARSCoV-2. However, its efficacy in moderate to severe COVID-19 remains uncertain, requiring further studies for clarification.

DIABETES & METABOLIC SYNDROME-CLINICAL RESEARCH & REVIEWS (2021)

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Article Pharmacology & Pharmacy

Identification of Plitidepsin as Potent Inhibitor of SARS-CoV-2-Induced Cytopathic Effect After a Drug Repurposing Screen

Jordi Rodon et al.

Summary: This study identified potential antiviral drugs for the treatment of COVID-19 by screening existing drugs approved for human use. Among the 72 antivirals tested, only 18% showed effective inhibition of viral replication, with Plitidepsin being the most promising candidate. Drug combinations showed no particular synergy, but did not reduce antiviral activity, potentially decreasing the emergence of resistant viruses.

FRONTIERS IN PHARMACOLOGY (2021)

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Article Chemistry, Medicinal

Small-Molecule Inhibitors of the Coronavirus Spike: ACE2 Protein- Protein Interaction as Blockers of Viral Attachment and Entry for SARS-CoV-2

Damir Bojadzic et al.

Summary: In this study, small-molecule inhibitors targeting the protein-protein interaction between SARS-CoV-2 and hACE2 were identified through screening a compound library focused on organic dyes. These inhibitors showed low micromolar activity and effectively blocked the interaction between the virus and cells in experiments. This provides a new approach for the prevention and treatment of viral infections.

ACS INFECTIOUS DISEASES (2021)

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Article Microbiology

Global Genomic Analysis of SARS-CoV-2 RNA Dependent RNA Polymerase Evolution and Antiviral Drug Resistance

Alfredo Mari et al.

Summary: Various antiviral treatments for COVID-19, including repurposed drugs, have been investigated. The RNA-dependent RNA polymerase of SARS-CoV-2 has been targeted by inhibitors like remdesivir, but potential resistance mutations are rare and unlikely to destabilize the polymerase. This suggests that monitoring for drug resistance during the pandemic is crucial for global efforts.

MICROORGANISMS (2021)

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Article Medicine, General & Internal

Effect of Early Treatment With Hydroxychloroquine or Lopinavir and Ritonavir on Risk of Hospitalization Among Patients With COVID-19 The TOGETHER Randomized Clinical Trial

Gilmar Reis et al.

Summary: This randomized clinical trial did not find any significant benefit in reducing COVID-19-associated hospitalization or other secondary clinical outcomes with hydroxychloroquine or lopinavir-ritonavir among high-risk outpatients.

JAMA NETWORK OPEN (2021)

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Article Biochemistry & Molecular Biology

Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp14 RNA cap methyltransferase

Souradeep Basu et al.

Summary: Researchers have identified four potential SARS-CoV-2 nsp14 inhibitors, all of which showed antiviral capacity in a cell-based model. Three of these compounds exhibited synergistic effects on viral replication with remdesivir.

BIOCHEMICAL JOURNAL (2021)

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Article Biochemistry & Molecular Biology

Coupling of N7-methyltransferase and 3′-5′ exoribonuclease with SARS-CoV-2 polymerase reveals mechanisms for capping and proofreading

Liming Yan et al.

Summary: The study presents the cryo-EM structure of the SARS-CoV-2 replication-transcription complex (RTC) Cap(0)-RTC, demonstrating the proofreading mechanism of nsp14 and the role of nsp10/nsp14 in the formation of the capping complex.

CELL (2021)

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Article Infectious Diseases

Optimal dose and safety of molnupiravir in patients with early SARS-CoV-2: a Phase I, open-label, dose-escalating, randomized controlled study

Saye H. Khoo et al.

Summary: The study found that molnupiravir is safe and well tolerated in treating early COVID-19 patients. A dose of 800mg twice daily for 5 days was recommended for Phase II evaluation.

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2021)

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Article Immunology

Molnupiravir Inhibits Replication of the Emerging SARS-CoV-2 Variants of Concern in a Hamster Infection Model

Rana Abdelnabi et al.

Summary: The emergence of SARS-CoV-2 variants of concern has worsened the COVID-19 pandemic, with current monoclonal antibodies and vaccines showing reduced efficacy against some of these variants. However, antivirals targeting conserved proteins of SARS-CoV-2 are likely to remain effective. Research on molnupiravir has shown effectiveness against different variants, highlighting its potential in combating current and future variants.

JOURNAL OF INFECTIOUS DISEASES (2021)

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Article Virology

Comparing the effectiveness of Atazanavir/Ritonavir/Dolutegravir/Hydroxychloroquine and Lopinavir/Ritonavir/Hydroxychloroquine treatment regimens in COVID-19 patients

Saeed Kalantari et al.

Summary: This study compared the effectiveness of Atazanavir/Dolutegravir/Hydroxychloroquine and Lopinavir/Ritonavir/Hydroxychloroquine treatment regimens in COVID-19 patients. The results indicated that the former regimen led to improvements in clinical and laboratory parameters in patients compared to the latter.

JOURNAL OF MEDICAL VIROLOGY (2021)

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Article Chemistry, Medicinal

In silico Studies on the Interaction Between Mpro and PLpro From SARS-CoV-2 and Ebselen, its Metabolites and Derivatives

Pablo Andrei Nogara et al.

Summary: This study simulates the interactions between Ebselen and its derivatives with Mpro and PLpro to find potential inhibitors of the SARS-CoV-2 proteases. Experimental data indicate that the thiol nucleophilic attack on selenium is more favorable for enzyme inhibition. Organoselenium molecules show promise as inhibitors of the SARS-CoV-2 proteases.

MOLECULAR INFORMATICS (2021)

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Article Biochemistry & Molecular Biology

Early treatment of COVID-19 with anakinra guided by soluble urokinase plasminogen receptor plasma levels: a double-blind, randomized controlled phase 3 trial

Evdoxia Kyriazopoulou et al.

Summary: The SAVE-MORE phase 3 study demonstrated the efficacy of anakinra, an IL-1 alpha/beta inhibitor, in patients with COVID-19 and high serum levels of soluble plasminogen activator receptor, showing significant reduction in clinical deterioration and decreased 28-day mortality.

NATURE MEDICINE (2021)

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Article Chemistry, Medicinal

Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate

Olga Bobileva et al.

Summary: This study designed potential SARS-CoV-2 MTase Nsp14 and Nsp16 inhibitors by using bioisosteric substitution of the cosubstrate SAM. Testing showed good inhibitory activity of five compounds. However, poor cell permeability was observed for all evaluated compounds.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

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Article Microbiology

In vitro selection of Remdesivir resistance suggests evolutionary predictability of SARS-CoV-2

Agnieszka M. Szemiel et al.

Summary: This study selected drug-resistant SARS-CoV-2 populations with decreased sensitivity to remdesivir (RDV) in vitro, identifying a mutation in NSP12 that decreases RDV sensitivity. There is no evidence of widespread transmission of RDV-resistant mutants among globally circulating SARS-CoV-2 variants. Additionally, emerging SARS-CoV-2 variants showed substitutions at Spike sites corresponding to those identified in vitro, indicating their potential to arise without immune selection.

PLOS PATHOGENS (2021)

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Article Immunology

Combination Treatment With Remdesivir and Ivermectin Exerts Highly Synergistic and Potent Antiviral Activity Against Murine Coronavirus Infection

Yu Ling Tan et al.

Summary: The study found that remdesivir monotherapy significantly inhibited live virus and viral RNA replication, while ivermectin treatment showed the highest selectivity index. Combination drug therapy exhibited strong synergistic effects, especially the combination of remdesivir and ivermectin showed the most significant reduction in live virus and viral RNA in infected macrophages.

FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY (2021)

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Article Chemistry, Medicinal

The Structure-Based Design of SARS-CoV-2 nsp14 Methyltransferase Ligands Yields Nanomolar Inhibitors

Tomas Otava et al.

Summary: The study focused on the design of inhibitors for SARS-CoV-2 nsp14 using a homology model based on its high similarity to SARS-CoV nsp14. The synthesized SAH derivatives showed unprecedented inhibitory activity against the crucial enzyme, with docking studies explaining their mechanism of action.

ACS INFECTIOUS DISEASES (2021)

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Article Medicine, General & Internal

Lopinavir/Ritonavir and Darunavir/Cobicistat in Hospitalized COVID-19 Patients: Findings From the Multicenter Italian CORIST Study

Augusto Di Castelnuovo et al.

Summary: In a multicenter observational study involving 33 Italian hospitals, the use of LPV/r treatment did not change death rate in COVID-19 patients, while DRV/c was associated with increased mortality. Within the limits of an observational study, these data do not support the use of LPV/r or DRV/c in COVID-19 patients.

FRONTIERS IN MEDICINE (2021)

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Article Medicine, General & Internal

被撤回的出版物: Proxalutamide Reduces the Rate of Hospitalization for COVID-19 Male Outpatients: A Randomized Double-Blinded Placebo-Controlled Trial (Publication with Expression of Concern. See vol. 8, 2022) (Retracted article. See vol. 9, 2022)

John McCoy et al.

Summary: The use of proxalutamide as an androgen receptor antagonist in men with COVID-19 has shown to significantly reduce the hospitalization rate, with a 91% reduction compared to usual care.

FRONTIERS IN MEDICINE (2021)

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Article Chemistry, Multidisciplinary

Inhibition of the 3CL Protease and SARS-CoV-2 Replication by Dalcetrapib

Eric J. Niesor et al.

Summary: The study revealed that Dalcetrapib could effectively inhibit SARS-CoV-2 viral replication by binding to the catalytic site of 3CL protease and stabilizing the protease-drug interaction. This finding paves the way for its clinical evaluation in the treatment of COVID-19.

ACS OMEGA (2021)

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Article Biochemistry & Molecular Biology

Azvudine is a thymus-homing anti-SARS-CoV-2 drug effective in treating COVID-19 patients

Jin-Lan Zhang et al.

Summary: FNC, a nucleoside analog, has shown activity against HIV-1 and SARS-CoV-2. Research suggests FNC's anti-viral effect is concentrated in the thymus, promoting immunity. Clinical trials have demonstrated oral FNC's ability to effectively cure COVID-19 patients.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

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Article Chemistry, Multidisciplinary

β-Blockers bearing hydroxyethylamine and hydroxyethylene as potential SARS-CoV-2 Mpro inhibitors: rational based design, in silico, in vitro, and SAR studies for lead optimization

Mohammed I. A. Hamed et al.

Summary: Through molecular docking and molecular dynamics simulations, researchers found that beta-adrenergic blockers have inhibitory effects on SARS-CoV-2, with Carvedilol and Nebivolol showing the most promising antiviral activities.

RSC ADVANCES (2021)

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Article Multidisciplinary Sciences

After the pandemic: perspectives on the future trajectory of COVID-19

Amalio Telenti et al.

Summary: This article discusses the future patterns of SARS-CoV-2 infection, the development of variants, and the implications for vaccine deployment. It suggests that the virus may become endemic fueled by pockets of susceptible individuals and waning immunity. Effective surveillance and response are crucial to prevent new epidemic or pandemic patterns.

NATURE (2021)

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Article Health Care Sciences & Services

A randomized, double-blind, placebo-controlled phase 1 trial of inhaled and intranasal niclosamide: A broad spectrum antiviral candidate for treatment of COVID-19

Vibeke Backer et al.

Summary: UNI91104, a promising candidate for the treatment of COVID-19 and other viral respiratory tract infections, is well-tolerated in healthy volunteers, demonstrating potential for further testing in patient trials.

LANCET REGIONAL HEALTH-EUROPE (2021)

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Article Chemistry, Multidisciplinary

In silico identification of potential SARS COV-2 2′-O-methyltransferase inhibitor: fragment-based screening approach and MM-PBSA calculations

Mahmoud A. El Hassab et al.

Summary: A new potential inhibitor for SARS CoV-2 2'-O-methyltransferase (nsp16), molecule AP-20, was proposed and demonstrated superior stability and binding free energy compared to Sinefungin in molecular dynamics simulations and MM-PBSA calculations. Experimental evaluations are recommended to further explore the potential inhibitory effect of AP-20 on the emerging COVID-19 spread. Additionally, in silico ADME profiling showed excellent safety and metabolic stability profile for AP-20.

RSC ADVANCES (2021)

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Article Medicine, General & Internal

Efficacy of the TMPRSS2 inhibitor camostat mesilate in patients hospitalized with Covid-19-a double-blind randomized controlled trial

Jesper D. Gunst et al.

Summary: This study evaluated the efficacy and safety of the TMPRSS2 inhibitor camostat mesilate in Covid-19 patients through a randomized controlled trial. The results showed that camostat mesilate treatment did not prolong time to clinical improvement and did not increase the occurrence of adverse events.

ECLINICALMEDICINE (2021)

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Article Multidisciplinary Sciences

Identification of SARS-CoV-2 inhibitors using lung and colonic organoids

Yuling Han et al.

Summary: Researchers have developed lung and colonic organoid models using human pluripotent stem cells, which demonstrate susceptibility to SARS-CoV-2 infection. These models are valuable for studying the infection of the virus and screening drugs, with potential therapeutic implications for COVID-19.

NATURE (2021)

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Article Pharmacology & Pharmacy

The broad spectrum antiviral ivermectin targets the host nuclear transport importin alpha/beta 1 heterodimer

Sundy N. Y. Yang et al.

ANTIVIRAL RESEARCH (2020)

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Letter Cell Biology

Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro

Manli Wang et al.

CELL RESEARCH (2020)

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Letter Immunology

Fusion mechanism of 2019-nCoV and fusion inhibitors targeting HR1 domain in spike protein

Shuai Xia et al.

CELLULAR & MOLECULAR IMMUNOLOGY (2020)

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Article Medicine, General & Internal

Genomic characterisation and epidemiology of 2019 novel coronavirus: implications for virus origins and receptor binding

Roujian Lu et al.

LANCET (2020)

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Article Medicine, General & Internal

Clinical features of patients infected with 2019 novel coronavirus in Wuhan, China

Chaolin Huang et al.

LANCET (2020)

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Article Multidisciplinary Sciences

A new coronavirus associated with human respiratory disease in China

Fan Wu et al.

NATURE (2020)

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Article Multidisciplinary Sciences

A pneumonia outbreak associated with a new coronavirus of probable bat origin

Peng Zhou et al.

NATURE (2020)

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Editorial Material Biotechnology & Applied Microbiology

Therapeutic options for the 2019 novel coronavirus (2019-nCoV)

Guangdi Li et al.

NATURE REVIEWS DRUG DISCOVERY (2020)

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Article Multidisciplinary Sciences

Cryo-EM structure of the 2019-nCoV spike in the prefusion conformation

Daniel Wrapp et al.

SCIENCE (2020)

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Article Biochemistry & Molecular Biology

Structural and Functional Basis of SARS-CoV-2 Entry by Using Human ACE2

Qihui Wang et al.

CELL (2020)

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Article Biochemistry & Molecular Biology

Structure, Function, and Antigenicity of the SARS-CoV-2 Spike Glycoprotein

Alexandra C. Walls et al.

CELL (2020)

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Article Biochemistry & Molecular Biology

SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor

Markus Hoffmann et al.

CELL (2020)

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Article Cell Biology

Inhibition of SARS-CoV-2 (previously 2019-nCoV) infection by a highly potent pan-coronavirus fusion inhibitor targeting its spike protein that harbors a high capacity to mediate membrane fusion

Shuai Xia et al.

CELL RESEARCH (2020)

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Article Cell Biology

The correlation between viral clearance and biochemical outcomes of 94 COVID-19 infected discharged patients

Jing Yuan et al.

INFLAMMATION RESEARCH (2020)

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Article Multidisciplinary Sciences

Effective treatment of severe COVID-19 patients with tocilizumab

Xiaoling Xu et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)

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Letter Infectious Diseases

Baricitinib therapy in COVID-19: A pilot study on safety and clinical impact

Fabrizio Cantini et al.

JOURNAL OF INFECTION (2020)

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Article Infectious Diseases

Arbidol combined with LPV/r versus LPV/r alone against Corona Virus Disease 2019: A retrospective cohort study

Lisi Deng et al.

JOURNAL OF INFECTION (2020)

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Article Multidisciplinary Sciences

Structure of the RNA-dependent RNA polymerase from COVID-19 virus

Yan Gao et al.

SCIENCE (2020)

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Article Multidisciplinary Sciences

Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors

Linlin Zhang et al.

SCIENCE (2020)

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Article Multidisciplinary Sciences

Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV

Xiuyuan Ou et al.

NATURE COMMUNICATIONS (2020)

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Article Medicine, General & Internal

Triple combination of interferon beta-1b, lopinavir-ritonavir, and ribavirin in the treatment of patients admitted to hospital with COVID-19: an open-label, randomised, phase 2 trial

Ivan Fan-Ngai Hung et al.

LANCET (2020)

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Article Immunology

Interferon-α2b Treatment for COVID-19

Qiong Zhou et al.

FRONTIERS IN IMMUNOLOGY (2020)

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Article Chemistry, Multidisciplinary

Research and Development on Therapeutic Agents and Vaccines for COVID-19 and Related Human Coronavirus Diseases

Cynthia Liu et al.

ACS CENTRAL SCIENCE (2020)

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Article Multidisciplinary Sciences

Proteomics of SARS-CoV-2-infected host cells reveals therapy targets

Denisa Bojkova et al.

NATURE (2020)

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Article Multidisciplinary Sciences

Structure of the SARS-CoV-2 spike receptor-binding domain bound to the ACE2 receptor

Jun Lan et al.

NATURE (2020)

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Article Multidisciplinary Sciences

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing

David E. Gordon et al.

NATURE (2020)

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Article Multidisciplinary Sciences

Structural basis of receptor recognition by SARS-CoV-2

Jian Shang et al.

NATURE (2020)

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Article Multidisciplinary Sciences

Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors

Zhenming Jin et al.

NATURE (2020)

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Letter Cell Biology

The anti-influenza virus drug, arbidol is an efficient inhibitor of SARS-CoV-2 in vitro

Xi Wang et al.

CELL DISCOVERY (2020)

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Letter Biochemistry & Molecular Biology

The QT interval in patients with COVID-19 treated with hydroxychloroquine and azithromycin

Ehud Chorin et al.

NATURE MEDICINE (2020)

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Article Engineering, Multidisciplinary

Experimental Treatment with Favipiravir for COVID-19: An Open-Label Control Study

Qingxian Cai et al.

ENGINEERING (2020)

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Article Medicine, General & Internal

Remdesivir for the Treatment of Covid-19-Final Report

John H. Beigel et al.

NEW ENGLAND JOURNAL OF MEDICINE (2020)

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Article Medicine, General & Internal

A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19

B. Cao et al.

NEW ENGLAND JOURNAL OF MEDICINE (2020)

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Article Medicine, General & Internal

Observational Study of Hydroxychloroquine in Hospitalized Patients with Covid-19

Joshua Geleris et al.

NEW ENGLAND JOURNAL OF MEDICINE (2020)

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Article Pharmacology & Pharmacy

Atazanavir, alone or in combination with ritonavir, inhibits SARS-CoV-2 replication and pro-inflammatory cytokine production

Natalia Fintelman-Rodrigues et al.

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2020)

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Article Pharmacology & Pharmacy

The FDA-approved drug ivermectin inhibits the replication of SARS-CoV-2 in vitro

Leon Caly et al.

ANTIVIRAL RESEARCH (2020)

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Review Pharmacology & Pharmacy

Current and future therapeutical approaches for COVID-19

Yongtao Duan et al.

DRUG DISCOVERY TODAY (2020)

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Article Oncology

Preclinical profile and phase I clinical trial of a novel androgen receptor antagonist GT0918 in castration-resistant prostate cancer

Tie Zhou et al.

EUROPEAN JOURNAL OF CANCER (2020)

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Article Biochemistry & Molecular Biology

Structural Basis for Helicase-Polymerase Coupling in the SARS-CoV-2 Replication-Transcription Complex

James Chen et al.

CELL (2020)

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Article Chemistry, Multidisciplinary

A Randomized, Open-Label, Controlled Clinical Trial of Azvudine Tablets in the Treatment of Mild and Common COVID-19, a Pilot Study

Zhigang Ren et al.

ADVANCED SCIENCE (2020)

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Review Medicine, General & Internal

Pathophysiology, Transmission, Diagnosis, and Treatment of Coronavirus Disease 2019 (COVID-19) A Review

W. Joost Wiersinga et al.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2020)

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Article Immunology

Antiviral Activity and Safety of Darunavir/Cobicistat for the Treatment of COVID-19

Jun Chen et al.

OPEN FORUM INFECTIOUS DISEASES (2020)

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Article Multidisciplinary Sciences

Structure-based virtual screening of phytochemicals and repurposing of FDA approved antiviral drugs unravels lead molecules as potential inhibitors of coronavirus 3C-like protease enzyme

Arun Bahadur Gurung et al.

JOURNAL OF KING SAUD UNIVERSITY SCIENCE (2020)

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Article Medicine, Research & Experimental

Ribavirin, Remdesivir, Sofosbuvir, Galidesivir, and Tenofovir against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study

Abdo A. Elfiky

LIFE SCIENCES (2020)

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Article Multidisciplinary Sciences

Chloroquine does not inhibit infection of human lung cells with SARS-CoV-2

Markus Hoffmann et al.

NATURE (2020)

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Article Multidisciplinary Sciences

Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing

Laura Riva et al.

NATURE (2020)

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Article Multidisciplinary Sciences

Hydroxychloroquine use against SARS-CoV-2 infection in non-human primates

Pauline Maisonnasse et al.

NATURE (2020)

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Article Multidisciplinary Sciences

Papain-like protease regulates SARS-CoV-2 viral spread and innate immunity

Donghyuk Shin et al.

NATURE (2020)

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Article Biochemistry & Molecular Biology

Mechanism and inhibition of the papain-like protease, PLpro, of SARS-CoV-2

Theresa Klemm et al.

EMBO JOURNAL (2020)

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Article Multidisciplinary Sciences

Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2

Yuan-Lin Kang et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)

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Article Multidisciplinary Sciences

Type I and III interferons disrupt lung epithelial repair during recovery from viral infection

Jack Major et al.

SCIENCE (2020)

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Article Multidisciplinary Sciences

Distinct conformational states of SARS-CoV-2 spike protein

Yongfei Cai et al.

SCIENCE (2020)

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Article Virology

The Anticoagulant Nafamostat Potently Inhibits SARS-CoV-2 S Protein-Mediated Fusion in a Cell Fusion Assay System and Viral Infection In Vitro in a Cell-Type-Dependent Manner

Mizuki Yamamoto et al.

VIRUSES-BASEL (2020)

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Article Multidisciplinary Sciences

Structural analysis of the SARS-CoV-2 methyltransferase complex involved in RNA cap creation bound to sinefungin

Petra Krafcikova et al.

NATURE COMMUNICATIONS (2020)

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Article Cell Biology

Furin Inhibitors Block SARS-CoV-2 Spike Protein Cleavage to Suppress Virus Production and Cytopathic Effects

Ya-Wen Cheng et al.

CELL REPORTS (2020)

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Article Multidisciplinary Sciences

Activity profiling and crystal structures of inhibitor-bound SARS-CoV-2 papain-like protease: A framework for anti-COVID-19 drug design

Wioletta Rut et al.

SCIENCE ADVANCES (2020)

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Article Cell & Tissue Engineering

Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men

Ryan M. Samuel et al.

CELL STEM CELL (2020)

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Article Medicine, Research & Experimental

Efficacy and Safety of Lopinavir/Ritonavir or Arbidol in Adult Patients with Mild/Moderate COVID-19: An Exploratory Randomized Controlled Trial

Yueping Li et al.

MED (2020)

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Article Multidisciplinary Sciences

Structure and inhibition of the SARS-CoV-2 main protease reveal strategy for developing dual inhibitors against Mpro and cathepsin L

Michael Dominic Sacco et al.

SCIENCE ADVANCES (2020)

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Article Chemistry, Medicinal

An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19

Jonathan H. Shrimp et al.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2020)

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Letter Biochemistry & Molecular Biology

Salvianolic acid C potently inhibits SARS-CoV-2 infection by blocking the formation of six-helix bundle core of spike protein

Chan Yang et al.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2020)

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Article Biochemistry & Molecular Biology

Predicting commercially available antiviral drugs that may act on the novel coronavirus (SARS-CoV-2) through a drug-target interaction deep learning model

Bo Ram Beck et al.

COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL (2020)

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Article Multidisciplinary Sciences

Structure of the SARS-CoV nsp12 polymerase bound to nsp7 and nsp8 co-factors

Robert N. Kirchdoerfer et al.

NATURE COMMUNICATIONS (2019)

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Article Virology

Small-Molecule Antiviral β-D-N4-Hydroxycytidine Inhibits a Proofreading-Intact Coronavirus with a High Genetic Barrier to Resistance

Maria L. Agostini et al.

JOURNAL OF VIROLOGY (2019)

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Article Cell Biology

Characterization of orally efficacious influenza drug with high resistance barrier in ferrets and human airway epithelia

Mart Toots et al.

SCIENCE TRANSLATIONAL MEDICINE (2019)

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Review Biotechnology & Applied Microbiology

Coronaviruses - drug discovery and therapeutic options

Alimuddin Zumla et al.

NATURE REVIEWS DRUG DISCOVERY (2016)

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Review Virology

Recent progress in the discovery of inhibitors targeting coronavirus proteases

Haofeng Wang et al.

VIROLOGICA SINICA (2016)

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Review Pharmacology & Pharmacy

The SARS-coronavirus papain-like protease: Structure, function and inhibition by designed antiviral compounds

Yahira M. Baez-Santos et al.

ANTIVIRAL RESEARCH (2015)

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Article Cell Biology

Suppressive effects of androgens on the immune system

Abhishek Trigunaite et al.

CELLULAR IMMUNOLOGY (2015)

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Article Immunology

Treatment With Lopinavir/Ritonavir or Interferon-β1b Improves Outcome of MERS-CoV Infection in a Nonhuman Primate Model of Common Marmoset

Jasper Fuk-Woo Chan et al.

JOURNAL OF INFECTIOUS DISEASES (2015)

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Review Pharmacology & Pharmacy

Nitazoxanide: A first-in-class broad-spectrum antiviral agent

Jean-Francois Rossignol

ANTIVIRAL RESEARCH (2014)

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Article Chemistry, Medicinal

X-ray Structural and Biological Evaluation of a Series of Potent and Highly Selective Inhibitors of Human Coronavirus Papain-like Proteases

Yahira M. Baez-Santos et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

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Article Infectious Diseases

Effect of nitazoxanide in adults and adolescents with acute uncomplicated influenza: a double-blind, randomised, placebo-controlled, phase 2b/3 trial

Jason Haffizulla et al.

LANCET INFECTIOUS DISEASES (2014)

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Article Oncology

The Androgen-Regulated Protease TMPRSS2 Activates a Proteolytic Cascade Involving Components of the Tumor Microenvironment and Promotes Prostate Cancer Metastasis

Jared M. Lucas et al.

CANCER DISCOVERY (2014)

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Article Cell Biology

The newly emerged SARS-Like coronavirus HCoV-EMC also has an Achilles' heel: current effective inhibitor targeting a 3C-like protease

Zhilin Ren et al.

PROTEIN & CELL (2013)

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Article Biochemistry & Molecular Biology

Pegylated interferon-α protects type 1 pneumocytes against SARS coronavirus infection in macaques

BL Haagmans et al.

NATURE MEDICINE (2004)

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Article Medicine, General & Internal

Interferon alfacon-1 plus corticosteroids in severe acute respiratory syndrome - A preliminary study

MR Loutfy et al.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2003)

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Article Multidisciplinary Sciences

The crystal structures of severe acute respiratory syndrome virus main protease and its complex with an inhibitor

HT Yang et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2003)

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Review Pharmacology & Pharmacy

Lopinavir/ritonavir - A review of its use in the management of HIV infection

RS Cvetkovic et al.

DRUGS (2003)

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Recent advances in small-molecular therapeutics for COVID-19

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