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SL MD4 Enzyme inhibitors as medicines
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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
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What causes the high blood pressure? angiotensin I angiotensin II + dipeptide ACE - Angiotensin Converting Enzyme Inactive Active – causes high blood pressure Need enzyme inhibitor
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Following the lead Venom of Brazilian Arrowhead Viper can kill by lowering blood pressure It contained several proteins which were ACE inhibitors But proteins are digested in the stomach
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Try Ass 9.
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Back to the lead compounds.. Active proteins from snake venom had the amino acid proline at the COOH end of the chain.
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After synthesising hundreds of compounds with proline in … Not a protein so can be taken orally!
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Try Ass 10.
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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
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