Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease

Effective, safe, and pharmacokinetically suitable drugs are urgently needed to curb the ongoing COVID-19 pandemic. The main protease or 3C-like protease (Mpro or 3CLpro) of SARS-CoV-2 is considered an important target to formulate potent drugs corresponding to its crucial role in virus replication a...

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Main Authors: Hylemariam Mihiretie Mengist, Daniel Mekonnen, Ahmed Mohammed, Ronghua Shi, Tengchuan Jin
Format: Article
Language:English
Published: Frontiers Media S.A. 2021-02-01
Series:Frontiers in Pharmacology
Subjects:
Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2020.630500/full
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spelling doaj-b35aa105a0854052b83214a328fd33b72021-02-01T10:03:25ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122021-02-011110.3389/fphar.2020.630500630500Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main ProteaseHylemariam Mihiretie Mengist0Hylemariam Mihiretie Mengist1Hylemariam Mihiretie Mengist2Daniel Mekonnen3Daniel Mekonnen4Ahmed Mohammed5Ronghua Shi6Tengchuan Jin7Tengchuan Jin8Tengchuan Jin9Department of Obstetrics and Gynecology, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, ChinaHefei National Laboratory for Physical Sciences at Microscale, Division of Life Sciences and Medicine, The CAS Key Laboratory of Innate Immunity and Chronic Disease, School of Basic Medical Sciences, University of Science and Technology of China, Hefei, ChinaDepartment of Medical Laboratory Science, College of Health Sciences, Debre Markos University, Debre Markos, EthiopiaHefei National Laboratory for Physical Sciences at Microscale, Division of Life Sciences and Medicine, The CAS Key Laboratory of Innate Immunity and Chronic Disease, School of Basic Medical Sciences, University of Science and Technology of China, Hefei, ChinaDepartment of Medical Laboratory Science, College of Health Science and Medicine, Bahir Dar University, Bahir Dar, EthiopiaHefei National Laboratory for Physical Sciences at Microscale, Division of Life Sciences and Medicine, The CAS Key Laboratory of Innate Immunity and Chronic Disease, School of Basic Medical Sciences, University of Science and Technology of China, Hefei, ChinaHefei National Laboratory for Physical Sciences at Microscale, Division of Life Sciences and Medicine, The CAS Key Laboratory of Innate Immunity and Chronic Disease, School of Basic Medical Sciences, University of Science and Technology of China, Hefei, ChinaDepartment of Obstetrics and Gynecology, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, ChinaHefei National Laboratory for Physical Sciences at Microscale, Division of Life Sciences and Medicine, The CAS Key Laboratory of Innate Immunity and Chronic Disease, School of Basic Medical Sciences, University of Science and Technology of China, Hefei, ChinaCAS Center for Excellence in Molecular Cell Science, Chinese Academy of Science, Shanghai, ChinaEffective, safe, and pharmacokinetically suitable drugs are urgently needed to curb the ongoing COVID-19 pandemic. The main protease or 3C-like protease (Mpro or 3CLpro) of SARS-CoV-2 is considered an important target to formulate potent drugs corresponding to its crucial role in virus replication and maturation in addition to its relatively conserved active site. Promising baseline data on the potency and safety of drugs targeting SARS-CoV-2 Mpro are currently available. However, preclinical and clinical data on the pharmacokinetic profiles of these drugs are very limited. This review discusses the potency, safety, and pharmacokinetic profiles of potential inhibitors of SARS-CoV-2 Mpro and forward directions on the development of future studies focusing on COVID-19 therapeutics.https://www.frontiersin.org/articles/10.3389/fphar.2020.630500/fullpotencysafetypharmacokineticsinhibitorsSARS-CoV-2main protease
collection DOAJ
language English
format Article
sources DOAJ
author Hylemariam Mihiretie Mengist
Hylemariam Mihiretie Mengist
Hylemariam Mihiretie Mengist
Daniel Mekonnen
Daniel Mekonnen
Ahmed Mohammed
Ronghua Shi
Tengchuan Jin
Tengchuan Jin
Tengchuan Jin
spellingShingle Hylemariam Mihiretie Mengist
Hylemariam Mihiretie Mengist
Hylemariam Mihiretie Mengist
Daniel Mekonnen
Daniel Mekonnen
Ahmed Mohammed
Ronghua Shi
Tengchuan Jin
Tengchuan Jin
Tengchuan Jin
Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
Frontiers in Pharmacology
potency
safety
pharmacokinetics
inhibitors
SARS-CoV-2
main protease
author_facet Hylemariam Mihiretie Mengist
Hylemariam Mihiretie Mengist
Hylemariam Mihiretie Mengist
Daniel Mekonnen
Daniel Mekonnen
Ahmed Mohammed
Ronghua Shi
Tengchuan Jin
Tengchuan Jin
Tengchuan Jin
author_sort Hylemariam Mihiretie Mengist
title Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
title_short Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
title_full Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
title_fullStr Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
title_full_unstemmed Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
title_sort potency, safety, and pharmacokinetic profiles of potential inhibitors targeting sars-cov-2 main protease
publisher Frontiers Media S.A.
series Frontiers in Pharmacology
issn 1663-9812
publishDate 2021-02-01
description Effective, safe, and pharmacokinetically suitable drugs are urgently needed to curb the ongoing COVID-19 pandemic. The main protease or 3C-like protease (Mpro or 3CLpro) of SARS-CoV-2 is considered an important target to formulate potent drugs corresponding to its crucial role in virus replication and maturation in addition to its relatively conserved active site. Promising baseline data on the potency and safety of drugs targeting SARS-CoV-2 Mpro are currently available. However, preclinical and clinical data on the pharmacokinetic profiles of these drugs are very limited. This review discusses the potency, safety, and pharmacokinetic profiles of potential inhibitors of SARS-CoV-2 Mpro and forward directions on the development of future studies focusing on COVID-19 therapeutics.
topic potency
safety
pharmacokinetics
inhibitors
SARS-CoV-2
main protease
url https://www.frontiersin.org/articles/10.3389/fphar.2020.630500/full
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