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Lesson 6 Inhibitors

Competitive inhibitors bind to the active site of an enzyme, preventing substrate binding. This effect can be overcome at high substrate concentrations as the substrate can outcompete the inhibitor. Non-competitive inhibitors bind elsewhere, inducing a conformational change that prevents substrate conversion. Increasing substrate concentration does not overcome this inhibition. Organophosphate insecticides irreversibly inhibit acetylcholinesterase, potentially causing permanent neurological effects. Ethanol treatment for ethylene glycol poisoning works by competitively inhibiting its breakdown, but is only effective if limited quantities were consumed initially. Feedback inhibition regulates metabolic pathways by having the end product inhibit the first enzyme to prevent overproduction.

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75 views12 pages

Lesson 6 Inhibitors

Competitive inhibitors bind to the active site of an enzyme, preventing substrate binding. This effect can be overcome at high substrate concentrations as the substrate can outcompete the inhibitor. Non-competitive inhibitors bind elsewhere, inducing a conformational change that prevents substrate conversion. Increasing substrate concentration does not overcome this inhibition. Organophosphate insecticides irreversibly inhibit acetylcholinesterase, potentially causing permanent neurological effects. Ethanol treatment for ethylene glycol poisoning works by competitively inhibiting its breakdown, but is only effective if limited quantities were consumed initially. Feedback inhibition regulates metabolic pathways by having the end product inhibit the first enzyme to prevent overproduction.

Uploaded by

tbrook2017
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPTX, PDF, TXT or read online on Scribd

?

theory
Collision ?
Denaturation ?
Denaturation ?
Denaturation

Active site availability

Substrate
availability
Enzyme Inhibition
Use diagrams to explain the effects of competitive and
non-competitive inhibitors on enzymes
Interpret graphs that show the effects of inhibitors on an
enzyme catalysed reaction
Reversible and irreversible inhibitors
• An inhibitor is any substance that slows down or stops an
enzyme catalysed reaction by affecting the enzyme in some way
Irreversible inhibitors
• Form covalent bonds with enzymes and inhibit them
permanently. If this happens the enzyme is completely
inactivated and the cell must make more of it
Reversible inhibitors
• These bind temporarily with enzymes, and their inhibitory effect
can be reversed by a change in the environment of the enzyme

• There are two types of reversible inhibitor you need to know


about – competitive and non-competitive
Competitive Inhibitors…
The presence of inhibitor molecules decreases the rate
of enzyme reactions by competing with the normal substrate for the
active site;

The effect of a
competitive
inhibitor can be
overcome.
At high
substrate
concentration,
maximum
reaction rate is
achieved
At low substrate concentrations, the rate
of reaction is reduced
in the presence of the inhibitor, the
inhibitor competes successfully for
the active site

maximum rate

The effect of the inhibitor


is overcome by very
high substrate concentrations
At high substrate concentrations,
the inhibitor is out-competed by the
substrate and the maximum rate of
reaction is achieved
Non-competitive Inhibitors…
This inhibitor molecule attaches to the enzyme at a position
away from the active site - known as an allosteric site
The inhibitor molecule changes the shape of the active site
preventing induced fit. The substrate cannot be converted into
product.
The effect of the inhibitor is not overcome by increasing the
substrate concentration.
Substrate binds to the enzyme when a non-competitive inhibitor is present
but cannot be converted to product. The inhibitor molecule changes the
shape of the active site preventing induced fit.
Substrate cannot be converted into product.

Maximum reaction rate never achieved -


the effect of the inhibitor cannot be
overcome by increasing the substrate
concentration
The effect is equivalent to lowering
enzyme concentration
Type of inhibition?
Organophosphates which are used in insecticides work
by inhibiting an enzyme which is crucial to the healthy
functioning of the nervous system.
Humans also contain the same enzyme and if poisoned
by organophosphates often develop ‘shakes’. These
symptoms can last for the rest of a person’s life.
Type of inhibition?
Ethylene glycol is found in antifreeze.
Ethylene glycol is broken down by enzymes in the body
to produce glycolic acid and oxalic acid which are both
toxic.
People suffering from ethylene glycol poisoning are
given ethanol which inhibits the enzyme responsible for
its breakdown.
However, if large quantities of ethylene glycol have
been consumed then this treatment no longer works.
Metabolic Pathways and Feedback
Inhibition
Metabolic pathways are often sequences of chemical reactions
each controlled by a specific enzyme
INHIBITS
enzyme enzyme enzyme enzyme
1 2 3 4

A B C D E
The initial is converted by a series of into the
substrate intermediate compounds final product

It is wasteful
When the end for a sequence
product of chemical
of the pathway reactions
begins to
to accumulate, it
continue
may act asifan
the end product
inhibitor of theisfirst
being produced
enzyme in theatpathway
a rate surplus
to requirements…
Further production of
the end product is
prevented.

Known as
FEEDBACK
INHIBITION

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