Development of Small-Molecule MERS-CoV Inhibitors

Effect of interferon alpha and cyclosporine treatment separately and in combination on Middle East Respiratory Syndrome Coronavirus (MERS-CoV) replication in a human in-vitro and ex-vivo culture model

(2018) H.S. Li et al.   ANTIVIRAL RESEARCH

Disulfiram can inhibit MERS and SARS coronavirus papain-like proteases via different modes

(2018) Min-Han Lin et al.   ANTIVIRAL RESEARCH

Broad-spectrum antiviral activity of the eIF4A inhibitor silvestrol against corona- and picornaviruses

(2018) Christin Müller et al.   ANTIVIRAL RESEARCH

Structure-guided design of potent and permeable inhibitors of MERS coronavirus 3CL protease that utilize a piperidine moiety as a novel design element

(2018) Anushka C. Galasiti Kankanamalage et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors

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

MERS-CoV pathogenesis and antiviral efficacy of licensed drugs in human monocyte-derived antigen-presenting cells

(2018) Yu Cong et al.   PLoS One

Saracatinib Inhibits Middle East Respiratory Syndrome-Coronavirus Replication In Vitro

(2018) Jin Shin et al.   Viruses-Basel

Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease

(2018) Maria L. Agostini et al.   mBio

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

Safe, high-throughput screening of natural compounds of MERS-CoV entry inhibitors using a pseudovirus expressing MERS-CoV spike protein

(2018) Ji Yeun Kim et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Broad-spectrum inhibition of common respiratory RNA viruses by a pyrimidine synthesis inhibitor with involvement of the host antiviral response

(2017) Nam Nam Cheung et al.   JOURNAL OF GENERAL VIROLOGY

X-ray Structure and Enzymatic Activity Profile of a Core Papain-like Protease of MERS Coronavirus with utility for structure-based drug design

(2017) Jozlyn R. Clasman et al.   Scientific Reports

Development of small-molecule viral inhibitors targeting various stages of the life cycle of emerging and re-emerging viruses

(2017) Xiaohuan Wang et al.   Frontiers of Medicine

Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors

(2016) Vathan Kumar et al.   BIOORGANIC & MEDICINAL CHEMISTRY

MERS-CoV spike protein: a key target for antivirals

(2016) Lanying Du et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Coronaviruses — drug discovery and therapeutic options

(2016) Alimuddin Zumla et al.   NATURE REVIEWS DRUG DISCOVERY

A novel peptide with potent and broad-spectrum antiviral activities against multiple respiratory viruses

(2016) Hanjun Zhao et al.   Scientific Reports

Inhibitor Recognition Specificity of MERS-CoV Papain-like Protease May Differ from That of SARS-CoV

(2015) Hyun Lee et al.   ACS Chemical Biology

Protease inhibitors targeting coronavirus and filovirus entry

(2015) Yanchen Zhou et al.   ANTIVIRAL RESEARCH

Design, synthesis and evaluation of a series of acyclic fleximer nucleoside analogues with anti-coronavirus activity

(2015) Hannah L. Peters et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Protective Effect of Intranasal Regimens Containing Peptidic Middle East Respiratory Syndrome Coronavirus Fusion Inhibitor Against MERS-CoV Infection

(2015) Rudragouda Channappanavar et al.   JOURNAL OF INFECTIOUS DISEASES

Characterization and Demonstration of the Value of a Lethal Mouse Model of Middle East Respiratory Syndrome Coronavirus Infection and Disease

(2015) Xinrong Tao et al.   JOURNAL OF VIROLOGY

ATP1A1-Mediated Src Signaling Inhibits Coronavirus Entry into Host Cells

(2015) Christine Burkard et al.   JOURNAL OF VIROLOGY

Intranasally administered peptidic viral fusion inhibitor protected hDPP4 transgenic mice from MERS-CoV infection

(2015) Shibo Jiang et al.   LANCET

The heptad repeat region is a major selection target in MERS-CoV and related coronaviruses

(2015) Diego Forni et al.   Scientific Reports

Structures of theMiddle East respiratory syndrome coronavirus3C-like protease reveal insights into substrate specificity

(2015) Danielle Needle et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Urgent development of effective therapeutic and prophylactic agents to control the emerging threat of Middle East respiratory syndrome (MERS)

(2015) Lu Lu et al.   Emerging Microbes & Infections

Clinical Course and Outcomes of Critically Ill Patients With Middle East Respiratory Syndrome Coronavirus Infection

(2014) Yaseen M. Arabi et al.   ANNALS OF INTERNAL MEDICINE

Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture

(2014) Adriaan H. de Wilde et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Testing of Middle East Respiratory Syndrome Coronavirus Replication Inhibitors for the Ability To Block Viral Entry

(2014) Qi Liu et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Evaluation of SSYA10-001 as a Replication Inhibitor of Severe Acute Respiratory Syndrome, Mouse Hepatitis, and Middle East Respiratory Syndrome Coronaviruses

(2014) Adeyemi O. Adedeji et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Repurposing of Clinically Developed Drugs for Treatment of Middle East Respiratory Syndrome Coronavirus Infection

(2014) Julie Dyall et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Structural Basis for Inactivation ofGiardia lambliaCarbamate Kinase by Disulfiram

(2014) Andrey Galkin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Blocking of Exchange Proteins Directly Activated by cAMP Leads to Reduced Replication of Middle East Respiratory Syndrome Coronavirus

(2014) X. Tao et al.   JOURNAL OF VIROLOGY

Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430

(2014) Travis K. Warren et al.   NATURE

Transmission of MERS-Coronavirus in Household Contacts

(2014) Christian Drosten et al.   NEW ENGLAND JOURNAL OF MEDICINE

Host cell entry of Middle East respiratory syndrome coronavirus after two-step, furin-mediated activation of the spike protein

(2014) Jean Kaoru Millet et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Middle East respiratory syndrome coronavirus (MERS-CoV) entry inhibitors targeting spike protein

(2014) Shuai Xia et al.   VIRUS RESEARCH

Spread, Circulation, and Evolution of the Middle East Respiratory Syndrome Coronavirus

(2014) M. Cotten et al.   mBio

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

(2014) Lu Lu et al.   Nature Communications

Targeting Membrane-Bound Viral RNA Synthesis Reveals Potent Inhibition of Diverse Coronaviruses Including the Middle East Respiratory Syndrome Virus

(2014) Anna Lundin et al.   PLoS Pathogens

Structural basis for catalysis and ubiquitin recognition by theSevere acute respiratory syndrome coronaviruspapain-like protease

(2014) Chi-Yuan Chou et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Disulfiram is a direct and potent inhibitor of human O6-methylguanine-DNA methyltransferase (MGMT) in brain tumor cells and mouse brain and markedly increases the alkylating DNA damage

(2013) A. Paranjpe et al.   CARCINOGENESIS

Proteolytic processing, deubiquitinase and interferon antagonist activities of Middle East respiratory syndrome coronavirus papain-like protease

(2013) X. Yang et al.   JOURNAL OF GENERAL VIROLOGY

Interferon-  and mycophenolic acid are potent inhibitors of Middle East respiratory syndrome coronavirus in cell-based assays

(2013) B. J. Hart et al.   JOURNAL OF GENERAL VIROLOGY

The emerging novel Middle East respiratory syndrome coronavirus: The “knowns” and “unknowns”

(2013) Jasper Fuk-Woo Chan et al.   JOURNAL OF THE FORMOSAN MEDICAL ASSOCIATION

Middle East Respiratory Syndrome Coronavirus Infection Mediated by the Transmembrane Serine Protease TMPRSS2

(2013) Kazuya Shirato et al.   JOURNAL OF VIROLOGY

TMPRSS2 Activates the Human Coronavirus 229E for Cathepsin-Independent Host Cell Entry and Is Expressed in Viral Target Cells in the Respiratory Epithelium

(2013) S. Bertram et al.   JOURNAL OF VIROLOGY

Structure of the Fusion Core and Inhibition of Fusion by a Heptad Repeat Peptide Derived from the S Protein of Middle East Respiratory Syndrome Coronavirus

(2013) J. Gao et al.   JOURNAL OF VIROLOGY

The Spike Protein of the Emerging Betacoronavirus EMC Uses a Novel Coronavirus Receptor for Entry, Can Be Activated by TMPRSS2, and Is Targeted by Neutralizing Antibodies

(2013) S. Gierer et al.   JOURNAL OF VIROLOGY

Assessing Activity and Inhibition of Middle East Respiratory Syndrome Coronavirus Papain-Like and 3C-Like Proteases Using Luciferase-Based Biosensors

(2013) A. Kilianski et al.   JOURNAL OF VIROLOGY

Middle East respiratory syndrome coronavirus (MERS-CoV): challenges in identifying its source and controlling its spread

(2013) Lu Lu et al.   MICROBES AND INFECTION

Dipeptidyl peptidase 4 is a functional receptor for the emerging human coronavirus-EMC

(2013) V. Stalin Raj et al.   NATURE

Treatment with interferon-α2b and ribavirin improves outcome in MERS-CoV–infected rhesus macaques

(2013) Darryl Falzarano et al.   NATURE MEDICINE

MERS-CoV papain-like protease has deISGylating and deubiquitinating activities

(2013) Anna M. Mielech et al.   VIROLOGY

A safe and convenient pseudovirus-based inhibition assay to detect neutralizing antibodies and screen for viral entry inhibitors against the novel human coronavirus MERS-CoV

(2013) Guangyu Zhao et al.   Virology Journal

Cell Host Response to Infection with Novel Human Coronavirus EMC Predicts Potential Antivirals and Important Differences with SARS Coronavirus

(2013) L. Josset et al.   mBio

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

(2013) Zhilin Ren et al.   Protein & Cell

Polyether ionophores—promising bioactive molecules for cancer therapy

(2012) Adam Huczyński   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

TMPRSS2 and TMPRSS4 Facilitate Trypsin-Independent Spread of Influenza Virus in Caco-2 Cells

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

Identification of Selective Inhibitors of Cancer Stem Cells by High-Throughput Screening

(2009) Piyush B. Gupta et al.   CELL

Two adjacent mutations on the dimer interface of SARS coronavirus 3C-like protease cause different conformational changes in crystal structure

(2009) Tiancen Hu et al.   VIROLOGY

Efficient Multiplication of Human Metapneumovirus in Vero Cells Expressing the Transmembrane Serine Protease TMPRSS2

(2008) Y. Shirogane et al.   JOURNAL OF VIROLOGY