The research progress of SARS-CoV-2 main protease inhibitors from 2020 to 2022

被引：66

作者：

Pang, Xiaojing ^{[1
]}

Liu, Yang ^{[1
]}

Li, Hua ^{[1
,2
]}

Chen, Lixia ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Wuya Coll Innovat, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China

[2] Fujian Univ Tradit Chinese Med, Inst Struct Pharmacol & TCM Chem Biol, Coll Pharm, Fuzhou 350122, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2023年 / 257卷

基金：

中国国家自然科学基金;

关键词：

COVID-19; SARS-CoV-2; M pro inhibitors; Drug repurposing; Drug design; COVALENT INHIBITORS; GENOME SEQUENCE; ACHILLES-HEEL; CORONAVIRUS; DISCOVERY; EBSELEN; IDENTIFICATION; REPLICATION; DESIGN; 3C;

D O I：

10.1016/j.ejmech.2023.115491

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The novel coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread worldwide. The main protease (Mpro) of SARS-CoV-2 plays a central role in viral replication and transcription and represents an attractive drug target for fighting COVID-19. Many SARS-CoV-2 Mpro inhibitors have been reported, including covalent and noncovalent inhibitors. The SARS-CoV-2 Mpro inhibitor PF-07321332 (Nirmatrelvir) designed by Pfizer has been put on the market. This paper briefly introduces the structural characteristics of SARS-CoV-2 Mpro and summarizes the research progress of SARS-CoV-2 Mpro inhibitors from the aspects of drug repurposing and drug design. These information will provide a basis for the drug development of treating the infection of SARS-CoV-2 and even other coronaviruses in the future.

引用

页数：20

共 107 条

[81]

Tomar S., J Biol Chem

[82] Screening and evaluation of approved drugs as inhibitors of main protease of SARS-CoV-2 [J].

Tripathi, Praveen Kumar ;

Upadhyay, Saurabh ;

Singh, Manju ;

Raghavendhar, Siva ;

Bhardwaj, Mohit ;

Sharma, Pradeep ;

Patel, Ashok Kumar .

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 2020, 164 :2622-2631

[83] S-217622, a 3CL Protease Inhibitor and Clinical Candidate for SARSCoV-2 [J].

Tyndall, Joel D. A. .

JOURNAL OF MEDICINAL CHEMISTRY, 2022, 65 (09) :6496-6498

[84] Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CLProtease Inhibitor Clinical Candidate for Treating COVID-19 [J].

Unoh, Yuto ;

Uehara, Shota ;

Nakahara, Kenji ;

Nobori, Haruaki ;

Yamatsu, Yukiko ;

Yamamoto, Shiho ;

Maruyama, Yuki ;

Taoda, Yoshiyuki ;

Kasamatsu, Koji ;

Suto, Takahiro ;

Kouki, Kensuke ;

Nakahashi, Atsufumi ;

Kawashima, Sho ;

Sanaki, Takao ;

Toba, Shinsuke ;

Uemura, Kentaro ;

Mizutare, Tohru ;

Ando, Shigeru ;

Sasaki, Michihito ;

Orba, Yasuko ;

Sawa, Hirofumi ;

Sato, Akihiko ;

Sato, Takafumi ;

Kato, Teruhisa ;

Tachibana, Yuki .

JOURNAL OF MEDICINAL CHEMISTRY, 2022, 65 (09) :6499-6512

[85] A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir [J].

Vankadara, Subramanyam ;

Dawson, Monique Danielle ;

Fong, Jia Yi ;

Oh, Qin Yao ;

Ang, Qi An ;

Liu, Boping ;

Chang, Hong Yun ;

Koh, Judice ;

Koh, Xiaoying ;

Tan, Qian Wen ;

Joy, Joma ;

Chia, Cheng San Brian .

ACS MEDICINAL CHEMISTRY LETTERS, 2022, 13 (08) :1345-1350

[86] Molecular properties that influence the oral bioavailability of drug candidates [J].

Veber, DF ;

Johnson, SR ;

Cheng, HY ;

Smith, BR ;

Ward, KW ;

Kopple, KD .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (12) :2615-2623

[87] Proton-Coupled Conformational Activation of SARS Coronavirus Main Proteases and Opportunity for Designing Small-Molecule Broad-Spectrum Targeted Covalent Inhibitors [J].

Verma, Neha ;

Henderson, Jack A. ;

Shen, Jana .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2020, 142 (52) :21883-21890

[88] Improved SARS-CoV-2 Mpro inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies [J].

Vuong, Wayne ;

Fischer, Conrad ;

Khan, Muhammad Bashir ;

van Belkum, Marco J. ;

Lamer, Tess ;

Willoughby, Kurtis D. ;

Lu, Jimmy ;

Arutyunova, Elena ;

Joyce, Michael A. ;

Saffran, Holly A. ;

Shields, Justin A. ;

Young, Howard S. ;

Nieman, James A. ;

Tyrrell, D. Lorne ;

Lemieux, M. Joanne ;

Vederas, John C. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 222

[89]

Wang H., EUR J MED CHEM, V238

[90]

Wang PL, 2018, J VIROL, V92, DOI [10.1128/jvi.00954-18, 10.1128/JVI.00954-18]

← 2 3 4 5 6 7 8 9 10 11 →