Transcript Slides for Chapter 6a

Enzyme Active Site
Fig. 13-08, p.413
HIV-1 Protease complexed with the inhibitor Crixivan (RED) made by Merck
Competitive inhibition of the Opioid receptor
Naloxone
Morphine
-A “Secondary Metabolite”
that comes from the Poppy
plant
-It binds our opioid
receptors triggering its
pharmacological response
Drug Discovery?
Naltrexone
Both of these compounds are examples of a
competitive inhibitor of our opioid receptors.
Used to treat Morphine (and other opioids)
overdose and addiction
More specifically they are:
Opioid receptor antagonists – Which are
compounds that bind a specific receptor, but
do not trigger a response (or similar
response).
What happens when chemists get
bored? Here is another…
Buprenorphine
or the IUPAC:
(2S)-2-[(-)-(5R,6R,7R,14S)9α-cyclopropylmethyl-4,5-epoxy6,14-ethano-3-hydroxy6-methoxymorphinan-7-yl]3,3-dimethylbutan-2-ol
Note for clarification:
Competitive inhibition = enzyme
Receptor antagonist = receptor that
can trigger a response.
But the drug discovery for these
molecules and how they bind are
the same!