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

Bepridil is potent against SARS-CoV-2 in vitro

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Disruption of disulfides within RBD of SARS‐CoV‐2 spike protein prevents fusion and represents a target for viral entry inhibition by registered drugs

(2021) Mateja Manček‐Keber et al.   FASEB JOURNAL

Study design of Dal-GenE, a pharmacogenetic trial targeting reduction of cardiovascular events with dalcetrapib

(2020) Jean-Claude Tardif et al.   AMERICAN HEART JOURNAL

Potential covalent drugs targeting the main protease of the SARS-CoV-2 coronavirus

(2020) Sen Liu et al.   BIOINFORMATICS

Potential Inhibitors for Novel Coronavirus Protease Identified by Virtual Screening of 606 Million Compounds

(2020) André Fischer et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Pharmacologic Treatments for Coronavirus Disease 2019 (COVID-19)

(2020) James M. Sanders et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

SARS-CoV-2 productively infects human gut enterocytes

(2020) Mart M. Lamers et al.   SCIENCE

Rapid repurposing of drugs for COVID-19

(2020) R. Kiplin Guy et al.   SCIENCE

Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease

(2020) Wenhao Dai et al.   SCIENCE

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

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Potential anti‐SARS‐CoV‐2 drug candidates identified through virtual screening of the ChEMBL database for compounds that target the main coronavirus protease

(2020) Motonori Tsuji   FEBS Open Bio

Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease

(2020) Chunlong Ma et al.   CELL RESEARCH

The molecular virology of Coronaviruses

(2020) Ella Hartenian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Relative Abundance of SARS-CoV-2 Entry Genes in the Enterocytes of the Lower Gastrointestinal Tract

(2020) Jaewon J. Lee et al.   Genes

Impact of Thiol–Disulfide Balance on the Binding of Covid-19 Spike Protein with Angiotensin-Converting Enzyme 2 Receptor

(2020) Sanchita Hati et al.   ACS Omega

Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication

(2020) Wayne Vuong et al.   Nature Communications

Clinical Pharmacokinetics and Pharmacodynamics of Dalcetrapib

(2018) Donald M. Black et al.   CLINICAL PHARMACOKINETICS

Discovery of Covalent Ligands via Noncovalent Docking by Dissecting Covalent Docking Based on a “Steric-Clashes Alleviating Receptor (SCAR)” Strategy

(2016) Yuanbao Ai et al.   Journal of Chemical Information and Modeling

An Overview of Severe Acute Respiratory Syndrome–Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy

(2016) Thanigaimalai Pillaiyar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacogenomic Determinants of the Cardiovascular Effects of DalcetrapibCLINICAL PERSPECTIVE

(2015) Jean-Claude Tardif et al.   Circulation-Cardiovascular Genetics

Pharmacogenomic Determinants of the Cardiovascular Effects of DalcetrapibCLINICAL PERSPECTIVE

(2015) Jean-Claude Tardif et al.   Circulation-Cardiovascular Genetics

Pharmacokinetics and disposition of dalcetrapib in rats and monkeys

(2014) Hiroaki Takubo et al.   XENOBIOTICA

Evidence for a role of CETP in HDL remodeling and cholesterol efflux: Role of cysteine 13 of CETP

(2013) Cyrille Maugeais et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Safety, Tolerability and Pharmacokinetics of Dalcetrapib Following Single and Multiple Ascending Doses in Healthy Subjects

(2013) Michael Derks et al.   CLINICAL DRUG INVESTIGATION

Solubility and stability of dalcetrapib in vehicles and biological media

(2012) Günter Gross et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

Evidence of a Drug–Drug Interaction Linked to Inhibition of Ester Hydrolysis by Orlistat

(2012) Darren Bentley et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Determination of dalcetrapib by liquid chromatography–tandem mass spectrometry

(2012) Katja Heinig et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Effects of Dalcetrapib in Patients with a Recent Acute Coronary Syndrome

(2012) Gregory G. Schwartz et al.   NEW ENGLAND JOURNAL OF MEDICINE

SwissDock, a protein-small molecule docking web service based on EADock DSS

(2011) A. Grosdidier et al.   NUCLEIC ACIDS RESEARCH

Open Babel: An open chemical toolbox

(2011) Noel M O'Boyle et al.   Journal of Cheminformatics

Mutation of Glu-166 Blocks the Substrate-Induced Dimerization of SARS Coronavirus Main Protease

(2010) Shu-Chun Cheng et al.   BIOPHYSICAL JOURNAL

Lack of effect of dalcetrapib on QT interval in healthy subjects following multiple dosing

(2010) Michael Derks et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

No clinically relevant drug–drug interactions when dalcetrapib is co-administered with atorvastatin

(2010) Michael Derks et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Biochemical characterization of cholesteryl ester transfer protein inhibitors

(2010) Mollie Ranalletta et al.   JOURNAL OF LIPID RESEARCH

Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport

(2010) Eric J. Niesor et al.   JOURNAL OF LIPID RESEARCH

A single-center, open-label, one-sequence study of dalcetrapib coadministered with ketoconazole, and an in vitro study of the S-methyl metabolite of dalcetrapib

(2009) Michael Derks et al.   CLINICAL THERAPEUTICS

Free Thiol Group of MD-2 as the Target for Inhibition of the Lipopolysaccharide-induced Cell Activation

(2009) Mateja Manček-Keber et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural bioinformatics analysis of free cysteines in protein environments

(2009) Sheau Ling Ho et al.   Journal of the Taiwan Institute of Chemical Engineers

Biophysical and Biochemical Approach to Locating an Inhibitor Binding Site on Cholesteryl Ester Transfer Protein

(2008) David Cunningham et al.   BIOCONJUGATE CHEMISTRY