Rational Drug Design

Last time General drug design How to shut down a particular enzyme Antibacterials- penicillin

THIS TIME: aNTIVIRALS How is this related to cancer? Some viruses cause cancer! Why are viruses harder to treat than bacteria? Virus mutate much more often

Mutation- treatment challenge? Remember how we found the structure of the protein before designing a drug for it? If the protein keeps changing the drug might not be effective. Must target proteins that are “conserved”- don’t mutate

Viruses Noncellular DNA covered in a “membrane”- mostly proteins that keep changing and lipids There are a couple proteins that don’t change- the H and N

‘H’ protein is needed for the virus to enter the host cell ‘N’ protein is needed to cut the virus away from the host cell

haemagglutinin (H) and neuraminidase (N) proteins Sequence is largely conserved during evolution because the proteins are so important Good targets for drug design Drug Zanamavir (marketed as Relenza) binds to the neuraminidase protein (N)