User:Eran Hodis/Sandbox: Difference between revisions
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Because of its important role in virus infectivity, several anti-viral drugs have been designed to target neuraminidase, including oseltamivir (Tamiflu) and zanamivir (Relenza). Unfortunately, by early 2009, 98% of influenza A/H1N1 strains in North America have become resistant to Tamiflu. Tamiflu binding to neuraminidase moves glutamate 276 towards histidine 274, making more room for Tamiflu to bind tightly (PDB entry [[2hu4]]). But, in a <scene name='User:Eran_Hodis/Sandbox/Bound_tamiflu/1'>common mutant</scene> (H274Y), a larger tyrosine replaces the smaller histidine 274, preventing glutamate 276 from moving to make room for Tamiflu, resulting in weaker drug binding and thus resistance (PDB entry [[3cl0]]). Luckily the H274Y neuraminidase mutant is still susceptible to Relenza, which is smaller than Tamiflu. | Because of its important role in virus infectivity, several anti-viral drugs have been designed to target neuraminidase, including oseltamivir (Tamiflu) and zanamivir (Relenza). Unfortunately, by early 2009, 98% of influenza A/H1N1 strains in North America have become resistant to Tamiflu. Tamiflu binding to neuraminidase moves glutamate 276 towards histidine 274, making more room for Tamiflu to bind tightly (PDB entry [[2hu4]]). But, in a <scene name='User:Eran_Hodis/Sandbox/Bound_tamiflu/1'>common mutant</scene> (H274Y), a larger tyrosine replaces the smaller histidine 274, preventing glutamate 276 from moving to make room for Tamiflu, resulting in weaker drug binding and thus resistance (PDB entry [[3cl0]]). Luckily the H274Y neuraminidase mutant is still susceptible to Relenza, which is smaller than Tamiflu. | ||
<quiz display=simple> | |||
{Which neuraminidase residue moves to make room for Tamiflu binding but cannot do so in the H274Y neuraminidase mutant? | |||
|type="[]"} | |||
- histidine 274 | |||
- serine 278 | |||
+ glutamate 276 | |||
- tyrosine 274 | |||
</quiz> | |||
