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SL MD4
Enzyme
inhibitors as
medicines
A bit like the antagonists!
• Noradrenaline
(neurotransmitter)
• Fits into receptor site
• Electrical impulse sent to
heart muscles
• Increases heart beat
• Bad for heart
• Antagonist (propanolol)
blocks receptor site
• Angiotensin I (substrate)
• Fits into active site of
enzyme (ACE)
• Changes it to angiotensin
II
• Increases blood pressure
• Causes heart attacks and
strokes
• ACE inhibitor (captopril)
blocks active site
What causes the high blood
pressure?
Need
enzyme
inhibitor
ACE - Angiotensin
Converting Enzyme
angiotensin I
Inactive

angiotensin II
Active –
causes
high
blood
pressure
+
dipeptide
Following the lead
But proteins
are digested
in the
stomach
Venom of
Brazilian
Arrowhead
Viper can kill
by lowering
blood pressure
It contained
several
proteins
which were
ACE
inhibitors
Try Ass 9.
Back to the lead compounds ..
Active proteins from
snake venom had the
amino acid proline at the
COOH end of the chain.
After synthesising hundreds of
compounds with proline in …
Not a protein so can
be taken orally!
Try Ass 10.
A bit like the antagonists!
• Noradrenaline
(neurotransmitter)
• Fits into receptor site
• Electrical impulse sent to
heart muscles
• Increases heart beat
• Bad for heart
• Antagonist (propanolol)
blocks receptor site
• Angiotensin I (substrate)
• Fits into active site of
enzyme (ACE)
• Changes it to angiotensin
II
• Increases blood pressure
• Causes heart attacks and
strokes
• ACE inhibitor (captopril)
blocks active site