The study identifies and optimizes dipeptidyl inhibitors of norovirus 3C-like protease that demonstrate in vivo efficacy in a murine model, providing a potential avenue for antinorovirus therapeutics.
Advances preclinical norovirus protease inhibitors; leaves open human translation from murine models.
Norovirus infection constitutes the primary cause of acute viral gastroenteritis. There are currently no vaccines or norovirus-specific antiviral therapeutics available for the management of norovirus infection. Norovirus 3C-like protease is essential for viral replication, consequently, inhibition of this enzyme is a fruitful avenue of investigation that may lead to the emergence of antinorovirus therapeutics. We describe herein the optimization of dipeptidyl inhibitors of norovirus 3C-like protease using iterative SAR, X-ray crystallographic, and enzyme and cell-based studies. We also demonstrate herein in vivo efficacy of an inhibitor using the murine model of norovirus infection.
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Kankanamalage et al. (2015) studied this question.
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