Selective covalent targeting of SARS-CoV-2 main protease by enantiopure chlorofluoroacetamide-Reference-Cited by-同舟云学术

Selective covalent targeting of SARS-CoV-2 main protease by enantiopure chlorofluoroacetamide

Published:2022 Issue:10 Volume:13 Page:3027-3034
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Yamane Daiki¹,Onitsuka Satsuki¹,Re Suyong²,Isogai Hikaru¹,Hamada Rui¹,Hiramoto Tadanari¹,Kawanishi Eiji¹^ORCID,Mizuguchi Kenji²³,Shindo Naoya¹^ORCID,Ojida Akio¹^ORCID

Affiliation:

1. Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan

2. Artificial Intelligence Center for Health and Biomedical Research, National Institute of Biomedical Innovation, Health and Nutrition, 7-6-8 Saito-Asagi, Ibaraki, Osaka 567-0085, Japan

3. Institute for Protein Research, Osaka University, 3-2 Yamadaoka, Suita, Osaka 565-0871, Japan

Abstract

Chlorofluoroacetamide (CFA) was used as the warhead for covalent targeting of SARS-CoV-2 Mpro. The chirality at CFA showed marked influence on inhibitory activity, suggesting stereospecific activation of CFA for cysteine modification in the protein.

Funder

Japan Society for the Promotion of Science

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/SC/D1SC06596C

Reference40 articles.

1. A new coronavirus associated with human respiratory disease in China

2. A pneumonia outbreak associated with a new coronavirus of probable bat origin

3. SARS-CoV-2 variants, spike mutations and immune escape