Imatinib (STI571) Inhibits the Expression of Angiotensin-Converting Enzyme 2 and Cell Entry of the SARS-CoV-2-Derived Pseudotyped Viral Particles.
Int J Mol Sci
; 22(13)2021 Jun 28.
Article
in English
| MEDLINE | ID: covidwho-1288900
ABSTRACT
A group of clinically approved cancer therapeutic tyrosine kinase inhibitors was screened to test their effects on the expression of angiotensin-converting enzyme 2 (ACE2), the cell surface receptor for SARS-CoV-2. Here, we show that the receptor tyrosine kinase inhibitor imatinib (also known as STI571, Gleevec) can inhibit the expression of the endogenous ACE2 gene at both the transcript and protein levels. Treatment with imatinib resulted in inhibition of cell entry of the viral pseudoparticles (Vpps) in cell culture. In FVB mice orally fed imatinib, tissue expression of ACE2 was reduced, specifically in the lungs and renal tubules, but not in the parenchyma of other organs such as the heart and intestine. Our finding suggests that receptor tyrosine kinases play a role in COVID-19 infection and can be therapeutic targets with combined treatments of the best conventional care of COVID-19.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Down-Regulation
/
Virus Internalization
/
Imatinib Mesylate
/
Angiotensin-Converting Enzyme 2
/
SARS-CoV-2
Type of study:
Prognostic study
Limits:
Animals
/
Female
/
Humans
Language:
English
Year:
2021
Document Type:
Article
Affiliation country:
Ijms22136938
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