Publications by authors named "Anna Paszti"
Article Synopsis
- In vitro models of animals can help test antiviral drugs against SARS-CoV-2, particularly inhibitors of the enzyme TMPRSS2.
- Researchers measured the effects of these inhibitors on the activity of the cytochrome P450 (CYP) 1A2 enzyme and assessed their toxicity using specific assays.
- Results showed significant impacts on CYP1A2 in various animal microsomes, with specific IC50 values indicating the potency of different inhibitors, and the importance of TMPRSS2 as a target for developing new antiviral treatments.
The interactions of four sulfonylated Phe(3-Am)-derived inhibitors (MI-432, MI-463, MI-482 and MI-1900) of type II transmembrane serine proteases (TTSP) such as transmembrane protease serine 2 (TMPRSS2) were examined with serum albumin and cytochrome P450 (CYP) isoenzymes. Complex formation with albumin was investigated using fluorescence spectroscopy. Furthermore, microsomal hepatic CYP1A2, 2C9, 2C19 and 3A4 activities in presence of these inhibitors were determined using fluorometric assays.
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