Molecular Playground/Relenza

From Proteopedia

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Relenza is an anti-influenza drug. It must be injected, whereas the more popular anti-influenza drug Tamiflu can be taken by mouth. However, many of the influenza viruses that cause disease in humans have developed resistance to Tamiflu. This is the result of widespread overuse of Tamiflu. Public health agencies in many countries have stockpiled Tamiflu at great expense, but these stockpiles are now of limited usefulness. Luckily the H1N1 swine flu that caused the pandemic starting in mid-2009 was sensitive to Tamiflu. However, it is only a matter of time before H1N1 also becomes resistant, and Relenza will then be the last resort.

spinqualitylabelsall models Influenza neuraminidase N1 mutant His274Tyr with Relenza bound (3ckz). Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Tamiflu and Relenza inhibit the neuraminidase protein in influenza, a protein enzyme that needs to function in order for the virus to spread. One of most common mutation that makes neuraminidase N1 resistant to inhibition by Tamiflu is His274Tyr (H274Y). At right is shown influenza neuraminidase N1 mutant H274Y bound to Relenza.

For more about this topic (and references to sources), please see

• Molecular Playground/Tamiflu (a brief article)
• Avian Influenza Neuraminidase, Tamiflu and Relenza (a detailed article)