Dimerized fusion inhibitor peptides targeting the HR1–HR2 interaction of SARS-CoV-2

Author:

Tsuji Kohei1ORCID,Baffour-Awuah Owusu Kofi1,Miura Yutaro1,Ishii Takahiro1,Shinohara Kouki1,Kobayakawa Takuya1ORCID,Emi Akino2,Nakano Takashi2,Suzuki Youichi2,Tamamura Hirokazu1ORCID

Affiliation:

1. Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU), Chiyoda-ku, Tokyo 101-0062, Japan

2. Department of Microbiology and Infection Control, Faculty of Medicine, Osaka Medical and Pharmaceutical University, Takatsuki, Osaka 569-8686, Japan

Abstract

C-Terminally dimerized HR2 peptides of SARS-CoV-2 showed significantly higher antiviral activity than the corresponding monomers. Our dimerization strategy of HIV-1 fusion inhibitors successfully facilitated the design of potent inhibitors of SARS-CoV-2.

Funder

Japan Society for the Promotion of Science

Japan Agency for Medical Research and Development

Astellas Foundation for Research on Metabolic Disorders

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

Reference39 articles.

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3. U.S. Food & Drug Administration , FDA approves first treatment for COVID-19 , https://www.fda.gov/news-events/pressannouncements/fda-approves-first-treatment-covid-19 , accessed on 2021-1-21

4. Merck and Ridgeback's Investigational Oral Antiviral Molnupiravir Reduced the Risk of Hospitalization or Death by Approximately 50% Compared to Placebo for Patients with Mild or Moderate COVID-19 in Positive Interim Analysis of Phase 3 Study , Press Release from Merck & Co., Inc. , 2021 , accessed on 2022-5-12

5. World Health Organization , WHO updates its treatment guidelines to include molnupiravir , March 3, 2022 , https://www.who.int/news/item/03-03-2022-molnupiravir , accessed on 2022-5-12

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