Carey & Akpan
This is the antiviral that was the topic of this review article
What is Tamiflu?
This was the viral strain studied by van der Vries et al.
What is 2009 H1N1?
This is the dissociation constant for the enzyme-inhibitor complex
What is KI?
This residue at position 247 is rotated by the I223R mutation
What is Serine?
Tamiflu is the brand name of this antiviral drug
What is Oseltamivir?
This class of antiviral was studied in van der Vries et al.
What are neuraminidase inhibitors?
Mutation had approximately a 2 fold increase in Km
What is I223R?
This type of interaction occurs between inhibitors such as Tamiflu and Zanamivir and the active site of the NA in influenza A viruses
What is hydrogen bonding?
These are the 2 organizations that have contradicting information about Tamiflu
What are the CDC and FDA?
Isoleucine at position 223 is mutated to this residue in the mutant H1N1 viral strain
What is arginine?
Had the highest kinetic values across the board
What is the double mutant strain I223R/H275Y?
This residue binds directly to inhibitors at position 277
What is Glutamic acid?
This is the target protein that Tamiflu is designed to inhibit
What is Neuraminidase?
This is the most frequently observed NA mutation in influenza viruses
What is H257Y?
This was the least effective mutation (lowest KI) at inhibiting Zanamivir binding
What is H275Y?
Group 1 NAs differ from group 2 NAs in this way
What are an extra cavity (150-loop) and are in open conformation when unbound to ligand
These are the 2 main contradicting points about Tamiflu effectiveness
What are reducing symptoms vs preventing complications?
these two methods were used to analyze inhibitor binding to mutated H1N1 strains
What are enzyme kinetics and x-ray crystallography?
The KI for oseltamivir increased by this proportion for the double mutant strain I223R/H275Y
What is 7500-fold?
This is the main mechanism by which mutation I223R resists inhibitor binding
What is by binding to S247 shrinking the hydrophobic pocket?