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DIST_0511_j.chembiol.2021.04.020

SARS-CoV-2 PLpro inhibitor identified for COVID-19

Jun 4, 2021 | 11:40 PM GMT

DISEASE CATEGORY: Infectious disease

INDICATION: Coronavirus

A Chinese Academy of Sciences team identified an inhibitor of SARS-CoV-2 PLpro that could treat COVID-19. An in vitro high-throughput screen of 35,360 compounds followed by crystallographic studies, structure-based optimization and docking studies yielded a methylpiperazine carboxamide-based compound that bound SARS-CoV-2 PLpro with a Kd of 2.6 µM. In HeLa cells, the compound inhibited viral replication with an IC50 of 182 nM and reduced cell death.

TARGET/MARKER/PATHWAY: SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro)

EXPERIMENTAL SYSTEM: In vitro; cell culture

LICENSING STATUS: Patent and licensing status unavailable

PUBLICATION DETAILS: Shan, H. et al. Cell Chem. Biol.; published online April 27, 2021

doi:10.1016/j.chembiol.2021.04.020

CONTACT: Zheng Zhang, Chinese Academy of Sciences, Shanghai, China

email: zhangzheng1975@aliyun.com

CONTACT: Ying Li, same affiliation as above

email: liying@sioc.ac.cn

CONTACT: Lifeng Pan, same affiliation as above

email: panlf@sioc.ac.cn

CONTACT: Li Tan, same affiliation as above

email: tanli@sioc.ac.cn

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