SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells

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

(2020) Shuai Xia et al.   Cellular & Molecular Immunology

A Review of Small Molecule Inhibitors and Functional Probes of Human Cathepsin L

(2020) Dibyendu Dana et al.   MOLECULES

A new coronavirus associated with human respiratory disease in China

(2020) Fan Wu et al.   NATURE

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

(2020) Peng Zhou et al.   NATURE

A Novel Coronavirus from Patients with Pneumonia in China, 2019

(2020) Na Zhu et al.   NEW ENGLAND JOURNAL OF MEDICINE

Structural basis for the recognition of the SARS-CoV-2 by full-length human ACE2

(2020) Renhong Yan et al.   SCIENCE

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

(2020) Daniel Wrapp et al.   SCIENCE

Evolution of the novel coronavirus from the ongoing Wuhan outbreak and modeling of its spike protein for risk of human transmission

(2020) Xintian Xu et al.   Science China-Life Sciences

Genomic characterization of the 2019 novel human-pathogenic coronavirus isolated from a patient with atypical pneumonia after visiting Wuhan

(2020) Jasper Fuk-Woo Chan et al.   Emerging Microbes & Infections

The species Severe acute respiratory syndrome-related coronavirus: classifying 2019-nCoV and naming it SARS-CoV-2

(2020)   Nature Microbiology

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

(2020) Alexandra C. Walls et al.   CELL

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

(2020) Markus Hoffmann et al.   CELL

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

(2020) Shuai Xia et al.   CELL RESEARCH

Off‐Label Therapies for COVID‐19—Are We All In This Together?

(2020) Jonathan D. Alpern et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

The anti‐HIV drug nelfinavir mesylate (Viracept) is a potent inhibitor of cell fusion caused by the SARSCoV‐2 spike (S) glycoprotein warranting further evaluation as an antiviral against COVID‐19 infections

(2020) Farhana Musarrat et al.   JOURNAL OF MEDICAL VIROLOGY

Phylogenetic Analysis and Structural Modeling of SARS-CoV-2 Spike Protein Reveals an Evolutionary Distinct and Proteolytically Sensitive Activation Loop

(2020) Javier A. Jaimes et al.   JOURNAL OF MOLECULAR BIOLOGY

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

(2020) Yuanmei Zhu et al.   JOURNAL OF VIROLOGY

COVID-19 in Europe: the Italian lesson

(2020) Andrea Saglietto et al.   LANCET

COVID-19 and Italy: what next?

(2020) Andrea Remuzzi et al.   LANCET

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

(2020) Jun Lan et al.   NATURE

Remdesivir for 5 or 10 Days in Patients with Severe Covid-19

(2020) Jason D. Goldman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Remdesivir for the Treatment of Covid-19 — Preliminary Report

(2020) John H. Beigel et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of Influenza A virus propagation by benzoselenoxanthenes stabilizing TMPRSS2 Gene G-quadruplex and hence down-regulating TMPRSS2 expression

(2020) Li-Wen Shen et al.   Scientific Reports

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

(2020) Cynthia Liu et al.   ACS Central Science

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

(2020) Mizuki Yamamoto et al.   Viruses-Basel

COVID-19 infection: Origin, transmission, and characteristics of human coronaviruses

(2020) Muhammad Adnan Shereen et al.   Journal of Advanced Research

TMPRSS2 and furin are both essential for proteolytic activation of SARS-CoV-2 in human airway cells

(2020) Dorothea Bestle et al.   Life Science Alliance

TMPRSS2 contributes to virus spread and immunopathology in the airways of murine models after coronavirus infection

(2019) Naoko Iwata-Yoshikawa et al.   JOURNAL OF VIROLOGY

Unexpected Receptor Functional Mimicry Elucidates Activation of Coronavirus Fusion

(2019) Alexandra C. Walls et al.   CELL

A pan-coronavirus fusion inhibitor targeting the HR1 domain of human coronavirus spike

(2019) Shuai Xia et al.   Science Advances

Wild-type human coronaviruses prefer cell-surface TMPRSS2 to endosomal cathepsins for cell entry

(2018) Kazuya Shirato et al.   VIROLOGY

De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery

(2018) Chao Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cryo-EM structure of the SARS coronavirus spike glycoprotein in complex with its host cell receptor ACE2

(2018) Wenfei Song et al.   PLoS Pathogens

Drug repurposing: progress, challenges and recommendations

(2018) Sudeep Pushpakom et al.   NATURE REVIEWS DRUG DISCOVERY

Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir

(2017) Nicholas A. Meanwell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Guidelines for the prevention and treatment of travelers’ diarrhea: a graded expert panel report

(2017) Mark S. Riddle et al.   JOURNAL OF TRAVEL MEDICINE

A Lipopeptide HIV-1/2 Fusion Inhibitor with Highly Potent In Vitro , Ex Vivo , and In Vivo Antiviral Activity

(2017) Huihui Chong et al.   JOURNAL OF VIROLOGY

Tectonic conformational changes of a coronavirus spike glycoprotein promote membrane fusion

(2017) Alexandra C. Walls et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Immunogenicity and structures of a rationally designed prefusion MERS-CoV spike antigen

(2017) Jesper Pallesen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cryo-EM structures of MERS-CoV and SARS-CoV spike glycoproteins reveal the dynamic receptor binding domains

(2017) Yuan Yuan et al.   Nature Communications

Identification of Nafamostat as a Potent Inhibitor of Middle East Respiratory Syndrome Coronavirus S Protein-Mediated Membrane Fusion Using the Split-Protein-Based Cell-Cell Fusion Assay

(2016) Mizuki Yamamoto et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Cathepsin B and L inhibitors: a patent review (2010 - present)

(2016) Yu-Yao Li et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Clinical Isolates of Human Coronavirus 229E Bypass the Endosome for Cell Entry

(2016) Kazuya Shirato et al.   JOURNAL OF VIROLOGY

Cryo-electron microscopy structure of a coronavirus spike glycoprotein trimer

(2016) Alexandra C. Walls et al.   NATURE

Protease inhibitors targeting coronavirus and filovirus entry

(2015) Yanchen Zhou et al.   ANTIVIRAL RESEARCH

Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy

(2015) Shivsharan B. Kharatmal et al.   NEUROPHARMACOLOGY

Peptide fusion inhibitors targeting the HIV-1 gp41: a patent review (2009 – 2014)

(2014) Dongmei Zhang et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Structure-based discovery of Middle East respiratory syndrome coronavirus fusion inhibitor

(2014) Lu Lu et al.   Nature Communications

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

(2014) J. M. Lucas et al.   Cancer Discovery

Proteolytic activation of the SARS-coronavirus spike protein: Cutting enzymes at the cutting edge of antiviral research

(2013) Graham Simmons et al.   ANTIVIRAL RESEARCH

Chemical–biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target

(2013) Jonathan W Choy et al.   Beilstein Journal of Organic Chemistry

Identification of the first synthetic inhibitors of the type II transmembrane serine protease TMPRSS2 suitable for inhibition of influenza virus activation

(2013) Daniela Meyer et al.   BIOCHEMICAL JOURNAL

Antagonism of the Interferon-Induced OAS-RNase L Pathway by Murine Coronavirus ns2 Protein Is Required for Virus Replication and Liver Pathology

(2012) Ling Zhao et al.   Cell Host & Microbe

Simultaneous Treatment of Human Bronchial Epithelial Cells with Serine and Cysteine Protease Inhibitors Prevents Severe Acute Respiratory Syndrome Coronavirus Entry

(2012) M. Kawase et al.   JOURNAL OF VIROLOGY

Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT

(2011) Frank Sielaff et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cathepsin S inhibitors: 2004 – 2010

(2011) Alice Lee-Dutra et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Evidence that TMPRSS2 Activates the Severe Acute Respiratory Syndrome Coronavirus Spike Protein for Membrane Fusion and Reduces Viral Control by the Humoral Immune Response

(2011) I. Glowacka et al.   JOURNAL OF VIROLOGY

Novel Peptidyl Aryl Vinyl Sulfones as Highly Potent and Selective Inhibitors of Cathepsins L and B

(2010) Laura Mendieta et al.   ChemMedChem

Molecular Docking of Cathepsin L Inhibitors in the Binding Site of Papain

(2010) Mary Pat Beavers et al.   Journal of Chemical Information and Modeling

Specialized roles for cysteine cathepsins in health and disease

(2010) Jochen Reiser et al.   JOURNAL OF CLINICAL INVESTIGATION

Identification of the First Low-Molecular-Weight Inhibitors of Matriptase-2

(2010) Mihiret Tekeste Sisay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis for reversible and irreversible inhibition of human cathepsin L by their respective dipeptidyl glyoxal and diazomethylketone inhibitors

(2010) Rajesh T. Shenoy et al.   JOURNAL OF STRUCTURAL BIOLOGY

A Transmembrane Serine Protease Is Linked to the Severe Acute Respiratory Syndrome Coronavirus Receptor and Activates Virus Entry

(2010) A. Shulla et al.   JOURNAL OF VIROLOGY

Efficient Activation of the Severe Acute Respiratory Syndrome Coronavirus Spike Protein by the Transmembrane Protease TMPRSS2

(2010) S. Matsuyama et al.   JOURNAL OF VIROLOGY

Cleavage of Influenza Virus Hemagglutinin by Airway Proteases TMPRSS2 and HAT Differs in Subcellular Localization and Susceptibility to Protease Inhibitors

(2010) E. Bottcher-Friebertshauser et al.   JOURNAL OF VIROLOGY

Targeting Cell Entry of Enveloped Viruses as an Antiviral Strategy

(2010) Elodie Teissier et al.   MOLECULES

Type II transmembrane serine proteases in cancer and viral infections

(2009) So-Young Choi et al.   TRENDS IN MOLECULAR MEDICINE

Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype

(2008) Michael C. Myers et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Reviews Of Anti‐infective Agents: Maraviroc: The First of a New Class of Antiretroviral Agents

(2008) Rodger D. MacArthur et al.   CLINICAL INFECTIOUS DISEASES

Type II transmembrane serine proteases in development and disease

(2007) R SZABO et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY