Τίτλος:
The discovery and development of transmembrane serine protease 2
(TMPRSS2) inhibitors as candidate drugs for the treatment of COVID-19
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
Introduction Severe Acute Respiratory Syndrome Coronavirus 2
(SARS-CoV-2) has caused the devastating pandemic named coronavirus
disease 2019 (COVID-19). Unfortunately, the discovery of antiviral
agents to combat COVID-19 is still an unmet need. Transmembrane serine
protease 2 (TMPRSS2) is an important mediator in viral infection and
thus, TMPRRS2 inhibitors may be attractive agents for COVID-19
treatment. Areas covered This review article discusses the role of
TMPRSS2 in SARS-CoV-2 cell entry and summarizes the inhibitors of
TMPRSS2 and their potential anti-SARS activity. Two known TMPRSS2
inhibitors, namely camostat and nafamostat, approved drugs for the
treatment of pancreatitis, are under clinical trials as potential drugs
against COVID-19. Expert opinion Due to the lack of the crystal
structure of TMPRSS2, homology models have been developed to study the
interactions of known inhibitors, including repurposed drugs, with the
enzyme. However, novel TMPRSS2 inhibitors have been identified through
high-throughput screening, and appropriate assays studying their in
vitro activity have been set up. The discovery of TMPRSS2MODIFIER LETTER
PRIMEs crystal structure will facilitate the rational design of novel
inhibitors and in vivo studies and clinical trials will give a clear
answer if TMPRSS2 inhibitors could be a new weapon against COVID-19.
Συγγραφείς:
Mantzourani, Christiana
Vasilakaki, Sofia
Gerogianni,
Velisaria-Eleni
Kokotos, George
Περιοδικό:
Expert Opinion on Drug Discovery
Εκδότης:
ROUTLEDGE JOURNALS, TAYLOR & FRANCIS LTD
Λέξεις-κλειδιά:
Clinical trials; COVID-19; inhibitors; SARS-CoV-2; transmembrane serine
protease 2 (TMPRSS2)
DOI:
10.1080/17460441.2022.2029843
