Literature DB >> 33597888

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

Hylemariam Mihiretie Mengist1,2,3, Daniel Mekonnen2,4, Ahmed Mohammed2, Ronghua Shi2, Tengchuan Jin1,2,5.   

Abstract

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.
Copyright © 2021 Mengist, Mekonnen, Mohammed, Shi and Jin.

Entities:  

Keywords:  COVID-19; SARS-CoV-2; inhibitors; main protease; pharmacokinetics; potency; safety

Year:  2021        PMID： 33597888      PMCID： PMC7883113          DOI： 10.3389/fphar.2020.630500

Source DB:  PubMed          Journal:  Front Pharmacol        ISSN： 1663-9812            Impact factor:   5.810


  11 in total

1.  Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.

Authors:  Chun-Hui Zhang; Krasimir A Spasov; Raquel A Reilly; Klarissa Hollander; Elizabeth A Stone; Joseph A Ippolito; Maria-Elena Liosi; Maya G Deshmukh; Julian Tirado-Rives; Shuo Zhang; Zhuobin Liang; Scott J Miller; Farren Isaacs; Brett D Lindenbach; Karen S Anderson; William L Jorgensen
Journal:  ACS Med Chem Lett       Date:  2021-07-14       Impact factor: 4.345

Review 2.  Beyond the vaccines: a glance at the small molecule and peptide-based anti-COVID19 arsenal.

Authors:  Kunal Nepali; Ram Sharma; Sachin Sharma; Amandeep Thakur; Jing-Ping Liou
Journal:  J Biomed Sci       Date:  2022-09-06       Impact factor: 12.771

3.  Withasomniferol C, a new potential SARS-CoV-2 main protease inhibitor from the Withania somnifera plant proposed by in silico approaches.

Authors:  Shivananada Kandagalla; Hrvoje Rimac; Krishnamoorthy Gurushankar; Jurica Novak; Maria Grishina; Vladimir Potemkin
Journal:  PeerJ       Date:  2022-06-02       Impact factor: 3.061

Review 4.  The SARS-CoV-2 main protease (Mpro): Structure, function, and emerging therapies for COVID-19.

Authors:  Qing Hu; Yuan Xiong; Guang-Hao Zhu; Ya-Ni Zhang; Yi-Wen Zhang; Ping Huang; Guang-Bo Ge
Journal:  MedComm (2020)       Date:  2022-07-14

5.  Re-purposing of hepatitis C virus FDA approved direct acting antivirals as potential SARS-CoV-2 protease inhibitors.

Authors:  Reaz Uddin; Khurshid Jalal; Kanwal Khan; Zaheer Ul-Haq
Journal:  J Mol Struct       Date:  2021-11-19       Impact factor: 3.196

Review 6.  Virus structure and structure-based antivirals.

Authors:  Zlatka Plavec; Ina Pöhner; Antti Poso; Sarah J Butcher
Journal:  Curr Opin Virol       Date:  2021-09-24       Impact factor: 7.121

7.  In Silico Drug Repositioning to Target the SARS-CoV-2 Main Protease as Covalent Inhibitors Employing a Combined Structure-Based Virtual Screening Strategy of Pharmacophore Models and Covalent Docking.

Authors:  Luis Heriberto Vázquez-Mendoza; Humberto L Mendoza-Figueroa; Juan Benjamín García-Vázquez; José Correa-Basurto; Jazmín García-Machorro
Journal:  Int J Mol Sci       Date:  2022-04-03       Impact factor: 5.923

Review 8.  Estrogen Receptor Modulators in Viral Infections Such as SARS-CoV-2: Therapeutic Consequences.

Authors:  Nikita Abramenko; Fréderic Vellieux; Petra Tesařová; Zdeněk Kejík; Robert Kaplánek; Lukáš Lacina; Barbora Dvořánková; Daniel Rösel; Jan Brábek; Adam Tesař; Milan Jakubek; Karel Smetana
Journal:  Int J Mol Sci       Date:  2021-06-18       Impact factor: 5.923

9.  Flavonoids in Ampelopsis grossedentata as covalent inhibitors of SARS-CoV-2 3CLpro: Inhibition potentials, covalent binding sites and inhibitory mechanisms.

Authors:  Yuan Xiong; Guang-Hao Zhu; Ya-Ni Zhang; Qing Hu; Hao-Nan Wang; Hao-Nan Yu; Xiao-Ya Qin; Xiao-Qing Guan; Yan-Wei Xiang; Hui Tang; Guang-Bo Ge
Journal:  Int J Biol Macromol       Date:  2021-07-29       Impact factor: 6.953

10.  Structure-guided design of a perampanel-derived pharmacophore targeting the SARS-CoV-2 main protease.

Authors:  Maya G Deshmukh; Joseph A Ippolito; Chun-Hui Zhang; Elizabeth A Stone; Raquel A Reilly; Scott J Miller; William L Jorgensen; Karen S Anderson
Journal:  Structure       Date:  2021-06-21       Impact factor: 5.006
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