Lecture 14 - HIV Protease Inhibitors Flashcards
Drugs work best when
Target non human factor
Any drugs that bind to multiple targets tend have
Adversities
Patients don’t want to take
HIV difficult because
Integrates its viral DNA (via RNA) into human cells
HIV protease (enzyme)
Helps virus mature
HIV protease enzyme
Homodimer
Aspartate (aspartyl) protease
Cleave long protein
Work on bonds phenyl proline or Tyr proline (Mammals don’t have this enzyme)
Good target
Enzymes
Catalyze reactions
Active site
Preferred substrates
Inhibited. Competitive / non competitive
Used to develop a virus specific drug
what do you Need to know to design an inhibitor?
active site and substrate:
HIV proteases are a type of
aspartate (aspartyl) protease.
Aspartate residues in
active site
what do 2 residues use to cleave the peptide bond in a one-step reaction?
water
HIV Protease is a homodimer formed of
2 identical amino acid chains
aspartate residues.
HIV proteases cleaves bonds between
Phenylalanine and Proline
Tyrosin and Proline
Apart from aspartate residues what other residues help position amino acid chain (S) by forming hydrophobic pockets for side chains?
S1, S2, S3 (on one chain)
and
S1’, S2’, S3’ (on the other chain)
What is the substrate?
HIV protease cleave long amino acid chain that then forms multiple smaller proteins that the HIV virus uses to replicate and infect other cells
What bond do you need to cut to cleave a protein?
Peptide bond
