Sandbox Erice 7: Difference between revisions

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<applet load='3cl0' size='300' frame='true' align='right' caption='Insert caption here' />
<applet load='3cl0' size='300' frame='true' align='right' caption='Insert caption here' />


Because of its important role in virus infectivity, several anti-viral drugs have been designed to target neuraminidase, including <scene name='Sandbox_Erice_7/Zoom_3cl0/1'>oseltamivir</scene> (Tamiflu) and zanamivir (Relenza). Oseltamavir binding to neuraminidase moves glutamate 276 towards histidine 274, making more room for oseltamavir to bind tightly (PDB entry [[2hu4]]). But, in a common mutant (H274Y), a larger tyrosine replaces the smaller histidine 274, preventing glutamate 276 from moving to make room for oseltamavir binding, resulting in weaker drug binding and thus resistance (PDB entry [[3cl0]]). Luckily the H274Y neuraminidase mutant is still susceptible to zanamivir, which is smaller than oseltamavir.
Because of its important role in virus infectivity, several anti-viral drugs have been designed to target neuraminidase, including <scene name='Sandbox_Erice_7/Zoom_3cl0/1'>oseltamivir</scene> (Tamiflu) and zanamivir (Relenza). Oseltamavir binding to neuraminidase moves glutamate 276 towards histidine 274, making more room for oseltamavir to bind tightly (PDB entry [[2hu4]]). But, in a common mutant (H274Y), a larger tyrosine replaces the smaller histidine 274, preventing glutamate 276 from moving to make room for oseltamavir binding, resulting in weaker drug binding and thus resistance (PDB entry [[3cl0]]). Luckily the H274Y neuraminidase mutant is still susceptible to zanamivir, which is smaller than oseltamavir <ref>PMID:18480754</ref>.
 
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