Litcius/Paper detail

Protease inhibitors targeting the main protease and papain-like protease of coronaviruses

Clemente Capasso, Alessio Nocentini, Claudiu T. Supuran

2020Expert Opinion on Therapeutic Patents37 citationsDOI

Abstract

INTRODUCTION: ) and the papain-like protease (PLP) are conserved among the three pathogens and started to be considered as exciting drug targets for developing antivirals. AREAS COVERED: We review the drug design landscape in the scientific and patent literature to design peptidomimetic and non-peptidomimetic protease inhibitors (PIs) targeting these proteins. EXPERT OPINION: The X-ray crystal structures of some of these proteases, alone and in complex with various inhibitors, were crucial for the discovery of effective such compounds, some of which also showed considerable antiviral activity and are considered preclinical candidates to fight these emerging infections, which in the case of Covid-19 already provoked an unprecedented worldwide pandemic.

Topics & Concepts

ProteasePapainVirologyCoronavirus disease 2019 (COVID-19)CoronavirusProteasesSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)TMPRSS22019-20 coronavirus outbreakEnzymeBiologyProtease inhibitor (pharmacology)MASP1MicrobiologyChemistryBiochemistryMedicineVirusSerine proteaseViral loadDiseasePathologyAntiretroviral therapyInfectious disease (medical specialty)OutbreakSARS-CoV-2 and COVID-19 ResearchViral gastroenteritis research and epidemiologyRNA Interference and Gene Delivery
Protease inhibitors targeting the main protease and papain-like protease of coronaviruses | Litcius