Key Metabolic Enzymes Involved in Remdesivir Activation in Human Lung Cells

Author:

Li Ruidong1,Liclican Albert1,Xu Yili1,Pitts Jared1,Niu Congrong1,Zhang Jingyu1,Kim Cynthia1,Zhao Xiaofeng1,Soohoo Daniel1,Babusis Darius1,Yue Qin1,Ma Bin1,Murray Bernard P.1,Subramanian Raju1,Xie Xuping2ORCID,Zou Jing2,Bilello John P.1,Li Li1,Schultz Brian E.1,Sakowicz Roman1,Smith Bill J.1,Shi Pei-Yong2,Murakami Eisuke1,Feng Joy Y.1ORCID

Affiliation:

1. Gilead Sciences, Inc., Foster City, California, USA

2. Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, Texas, USA

Abstract

Remdesivir (RDV; GS-5734, Veklury), the first FDA-approved antiviral to treat COVID-19, is a single-diastereomer monophosphoramidate prodrug of an adenosine analogue. RDV is taken up in the target cells and metabolized in multiple steps to form the active nucleoside triphosphate (TP) (GS-443902), which, in turn, acts as a potent and selective inhibitor of multiple viral RNA polymerases.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

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