Researchers at St. Jude have identified novel small molecules that target RNA dependent RNA polymerase. These 4,5-dihydroxypyrimdines bind to the PA(N) endonuclease active site and act as anti-influenza inhibitors. These broad-spectrum anti-viral, pyrimidinone compounds can be developed to treat and prevent influenza.
In the event of a pandemic, antiviral drugs and non-pharmaceutical means of controlling infections are the first line defense. Currently, there are two antiviral drug options for treating influenza: M2 ion channel blockers, such as amantadines that block endocytosis and fusion of cells or the use of neuraminidase inhibitors such as oseltamivir and zanamivir that block viral release. However, amantadine has become very ineffective as a treatment, and oseltamivir seems to require much higher doses to be effective. Therefore, a novel therapeutic could offer substantial benefit.
Influenza, therapeutic, small molecule, inhibitor, RNA
Granted Patents or Published Applications
US Patent 9,328,075
Related Scientific References
Baughman BM, Jake Slavish P, DuBois RM, Boyd VA, White SW, Webb TR; Identification of influenza endonuclease inhibitors using a novel fluorescence polarization assay; ACS Chem Biol. 2012 Mar 16;7(3):526-34.
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