Transcript Rational Drug Design

RATIONAL DRUG DESIGN
LAST TIME
General drug design
 How to shut down a particular enzyme
 Antibacterials- penicillin
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THIS TIME: ANTIVIRALS
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How is this related to cancer?
 Some
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viruses cause cancer!
Why are viruses harder to treat than bacteria?
 Virus
mutate much more often
MUTATION- TREATMENT CHALLENGE?
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Remember how we found the structure of the
protein before designing a drug for it?
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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 changethe 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)
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