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Cell entry mechanisms of SARS-CoV-2 Open
Significance A key to curbing SARS-CoV-2 is to understand how it enters cells. SARS-CoV-2 and SARS-CoV both use human ACE2 as entry receptor and human proteases as entry activators. Using biochemical and pseudovirus entry assays and SARS-C…
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Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors Open
The coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome–coronavirus 2 (SARS-CoV-2) is a global health emergency. An attractive drug target among coronaviruses is the main protease (M pro , also called 3…
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Neuropilin-1 facilitates SARS-CoV-2 cell entry and infectivity Open
Another host factor for SARS-CoV-2 Virus-host interactions determine cellular entry and spreading in tissues. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and the earlier SARS-CoV use angiotensin-converting enzyme 2 (ACE2) …
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Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease Open
Promising antiviral protease inhibitors With no vaccine or proven effective drug against the virus that causes coronavirus disease 2019 (COVID-19), scientists are racing to find clinical antiviral treatments. A promising drug target is the…
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Neuropilin-1 is a host factor for SARS-CoV-2 infection Open
Another host factor for SARS-CoV-2 Virus-host interactions determine cellular entry and spreading in tissues. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and the earlier SARS-CoV use angiotensin-converting enzyme 2 (ACE2) …
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TMPRSS2 and furin are both essential for proteolytic activation of SARS-CoV-2 in human airway cells Open
The novel emerged SARS-CoV-2 has rapidly spread around the world causing acute infection of the respiratory tract (COVID-19) that can result in severe disease and lethality. For SARS-CoV-2 to enter cells, its surface glycoprotein spike (S)…
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An Overview of Severe Acute Respiratory Syndrome–Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy Open
Severe acute respiratory syndrome (SARS) is caused by a newly emerged coronavirus that infected more than 8000 individuals and resulted in more than 800 (10-15%) fatalities in 2003. The causative agent of SARS has been identified as a nove…
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The novel coronavirus 2019 (2019-nCoV) uses the SARS-coronavirus receptor ACE2 and the cellular protease TMPRSS2 for entry into target cells Open
The emergence of a novel, highly pathogenic coronavirus, 2019-nCoV, in China, and its rapid national and international spread pose a global health emergency. Coronaviruses use their spike proteins to select and enter target cells and insig…
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Matrix Metalloproteinase-9 (MMP-9) as a Cancer Biomarker and MMP-9 Biosensors: Recent Advances Open
As one of the most widely investigated matrix metalloproteinases (MMPs), MMP-9 is a significant protease which plays vital roles in many biological processes. MMP-9 can cleave many extracellular matrix (ECM) proteins to regulate ECM remode…
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Inhibition of SARS-CoV 3CL protease by flavonoids Open
There were severe panics caused by Severe Acute Respiratory Syndrome (SARS) and Middle-East Respiratory Syndrome-Coronavirus. Therefore, researches targeting these viruses have been required. Coronaviruses (CoVs) have been rising targets o…
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A Review and Database of Snake Venom Proteomes Open
Advances in the last decade combining transcriptomics with established proteomics methods have made possible rapid identification and quantification of protein families in snake venoms. Although over 100 studies have been published, the va…
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Intracellular Targeting Mechanisms by Antimicrobial Peptides Open
Antimicrobial peptides (AMPs) are expressed in various living organisms as first-line host defenses against potential harmful encounters in their surroundings. AMPs are short polycationic peptides exhibiting various antimicrobial activitie…
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Digestive system is a potential route of COVID-19: an analysis of single-cell coexpression pattern of key proteins in viral entry process Open
Objective Since December 2019, a newly identified coronavirus (severe acute respiratory syndrome coronavirus (SARS-CoV-2)) has caused outbreaks of pneumonia in Wuhan, China. SARS-CoV-2 enters host cells via cell receptor ACE II (ACE2) and …
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Rapid Identification of Potential Inhibitors of SARS‐CoV‐2 Main Protease by Deep Docking of 1.3 Billion Compounds Open
The recently emerged 2019 Novel Coronavirus (SARS‐CoV‐2) and associated COVID‐19 disease cause serious or even fatal respiratory tract infection and yet no approved therapeutics or effective treatment is currently available to effectively …
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Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19 Open
The novel coronavirus disease COVID-19 that emerged in 2019 is caused by the virus SARS CoV-2 and named for its close genetic similarity to SARS CoV-1 that caused severe acute respiratory syndrome (SARS) in 2002. Both SARS coronavirus geno…
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Nafamostat Mesylate Blocks Activation of SARS-CoV-2: New Treatment Option for COVID-19 Open
Funder: \n Bundesministerium für Bildung und Forschung\n https://doi.org/10.13039/501100002347
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Activity profiling and crystal structures of inhibitor-bound SARS-CoV-2 papain-like protease: A framework for anti–COVID-19 drug design Open
A multidisciplinary approach yields novel inhibitors and reveals substrate specificity, structure, and mechanisms of CoV-2 PLpro.
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Prediction of the SARS-CoV-2 (2019-nCoV) 3C-like protease (3CLpro) structure: virtual screening reveals velpatasvir, ledipasvir, and other drug repurposing candidates Open
We prepared the three-dimensional model of the SARS-CoV-2 (aka 2019-nCoV) 3C-like protease (3CL pro ) using the crystal structure of the highly similar (96% identity) ortholog from the SARS-CoV. All residues involved in the catalysis, subs…
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Role of Structural and Non-Structural Proteins and Therapeutic Targets of SARS-CoV-2 for COVID-19 Open
Coronavirus belongs to the family of Coronaviridae, comprising single-stranded, positive-sense RNA genome (+ ssRNA) of around 26 to 32 kilobases, and has been known to cause infection to a myriad of mammalian hosts, such as humans, cats, b…
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SARS-CoV-2 M <sup>pro</sup> inhibitors with antiviral activity in a transgenic mouse model Open
Targeting the SARS-CoV-2 main protease Vaccines are an important tool in the fight against COVID-19, but developing antiviral drugs is also a high priority, especially with the rise of variants that may partially evade vaccines. The viral …
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Multiple pathways for SARS-CoV-2 resistance to nirmatrelvir Open
Nirmatrelvir, an oral antiviral targeting the 3CL protease of SARS-CoV-2, has been demonstrated to be clinically useful against COVID-19 (refs. 1,2 ). However, because SARS-CoV-2 has evolved to become resistant to other therapeutic modalit…
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Nanocaged enzymes with enhanced catalytic activity and increased stability against protease digestion Open
Cells routinely compartmentalize enzymes for enhanced efficiency of their metabolic pathways. Here we report a general approach to construct DNA nanocaged enzymes for enhancing catalytic activity and stability. Nanocaged enzymes are realiz…
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Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS Open
HIV-1 protease inhibitors continue to play an important role in the treatment of HIV/AIDS, transforming this deadly ailment into a more manageable chronic infection. Over the years, intensive research has led to a variety of approved prote…
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Computational Design of ACE2-Based Peptide Inhibitors of SARS-CoV-2 Open
Peptide inhibitors against the SARS-CoV-2 coronavirus, currently causing a worldwide pandemic, are designed and simulated. The inhibitors are mostly formed by two sequential self-supporting α-helices (bundle) extracted from the protease do…
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Gasdermin D Exerts Anti-inflammatory Effects by Promoting Neutrophil Death Open
Gasdermin D (GSDMD) is considered a proinflammatory factor that mediates pyroptosis in macrophages to protect hosts from intracellular bacteria. Here, we reveal that GSDMD deficiency paradoxically augmented host responses to extracellular …
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Structure and inhibition of the SARS-CoV-2 main protease reveal strategy for developing dual inhibitors against M <sup>pro</sup> and cathepsin L Open
X-ray crystal structures of SARS-CoV-2 M pro with dual inhibitors provide a new direction for the designing of COVID-19 antivirals.
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Analysis of 138 pathogenic mutations in presenilin-1 on the in vitro production of Aβ42 and Aβ40 peptides by γ-secretase Open
Significance Alzheimer’s disease (AD) is the most common form of dementia, but the cause of AD remains poorly understood. Using highly purified recombinant γ-secretase, we examined the effect of 138 AD-derived presenilin-1 (PS1) mutations …
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An investigation into the identification of potential inhibitors of SARS-CoV-2 main protease using molecular docking study Open
A new strain of a novel infectious disease affecting millions of people, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has recently been declared as a pandemic by the World Health Organization (WHO). Currently, sev…
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Drug repurposing for coronavirus (COVID-19): <i>in silico</i> screening of known drugs against coronavirus 3CL hydrolase and protease enzymes Open
In December 2019, COVID-19 epidemic was described in Wuhan, China, and the infection has spread widely affecting hundreds of thousands. Herein, an effort was made to identify commercially available drugs in order to repurpose them against …
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Psychrophilic proteases dramatically reduce single cell RNA-seq artifacts: A molecular atlas of kidney development Open
Single cell RNA-seq is a powerful methodology. Nevertheless there are important limitations, including the technical challenges of breaking down an organ or tissue into a single cell suspension. Invariably this has required enzymatic incub…