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Progress in Developing Inhibitors of SARS-CoV-2 3C-Like Protease.
Li, Qingxin; Kang, CongBao.
  • Li Q; Guangdong Provincial Engineering Laboratory of Biomass High Value Utilization, Institute of Bioengineering, Guangdong Academy of Sciences, Guangzhou 510316, China.
  • Kang C; Experimental Drug Development Centre (EDDC), Agency for Science, Technology and Research (A*STAR), 10 Biopolis Road, Chromos, #05-01, Singapore 138670, Singapore.
Microorganisms ; 8(8)2020 Aug 18.
Article in English | MEDLINE | ID: covidwho-854167
Semantic information from SemMedBD (by NLM)
1. 2019 novel coronavirus CAUSES COVID-19
Subject
2019 novel coronavirus
Predicate
CAUSES
Object
COVID-19
2. Viral Genome INTERACTS_WITH Polyproteins
Subject
Viral Genome
Predicate
INTERACTS_WITH
Object
Polyproteins
3. Enzymes AFFECTS Virus Replication
Subject
Enzymes
Predicate
AFFECTS
Object
Virus Replication
4. Peptide Hydrolases PART_OF 2019 novel coronavirus
Subject
Peptide Hydrolases
Predicate
PART_OF
Object
2019 novel coronavirus
5. Antiviral Agents TREATS COVID-19
Subject
Antiviral Agents
Predicate
TREATS
Object
COVID-19
6. 2019 novel coronavirus CAUSES COVID-19
Subject
2019 novel coronavirus
Predicate
CAUSES
Object
COVID-19
7. Viral Genome INTERACTS_WITH Polyproteins
Subject
Viral Genome
Predicate
INTERACTS_WITH
Object
Polyproteins
8. Enzymes AFFECTS Virus Replication
Subject
Enzymes
Predicate
AFFECTS
Object
Virus Replication
9. Peptide Hydrolases PART_OF 2019 novel coronavirus
Subject
Peptide Hydrolases
Predicate
PART_OF
Object
2019 novel coronavirus
10. Antiviral Agents TREATS COVID-19
Subject
Antiviral Agents
Predicate
TREATS
Object
COVID-19
ABSTRACT
Coronavirus disease 2019 (COVID-19) is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The viral outbreak started in late 2019 and rapidly became a serious health threat to the global population. COVID-19 was declared a pandemic by the World Health Organization in March 2020. Several therapeutic options have been adopted to prevent the spread of the virus. Although vaccines have been developed, antivirals are still needed to combat the infection of this virus. SARS-CoV-2 is an enveloped virus, and its genome encodes polyproteins that can be processed into structural and nonstructural proteins. Maturation of viral proteins requires cleavages by proteases. Therefore, the main protease (3 chymotrypsin-like protease (3CLpro) or Mpro) encoded by the viral genome is an attractive drug target because it plays an important role in cleaving viral polyproteins into functional proteins. Inhibiting this enzyme is an efficient strategy to block viral replication. Structural studies provide valuable insight into the function of this protease and structural basis for rational inhibitor design. In this review, we describe structural studies on the main protease of SARS-CoV-2. The strategies applied in developing inhibitors of the main protease of SARS-CoV-2 and currently available protein inhibitors are summarized. Due to the availability of high-resolution structures, structure-guided drug design will play an important role in developing antivirals. The availability of high-resolution structures, potent peptidic inhibitors, and diverse compound scaffolds indicate the feasibility of developing potent protease inhibitors as antivirals for COVID-19.
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Full text: Available Collection: International databases Database: MEDLINE Topics: Vaccines Language: English Year: 2020 Document Type: Article Affiliation country: Microorganisms8081250

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Full text: Available Collection: International databases Database: MEDLINE Topics: Vaccines Language: English Year: 2020 Document Type: Article Affiliation country: Microorganisms8081250