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Enzyme Inhibition: Types and Definitions

Enzyme inhibition is a regulatory mechanism in biochemistry where inhibitors decrease the catalytic activity of enzymes. There are several types of inhibition including reversible, irreversible, and allosteric inhibition. Reversible inhibitors noncovalently bind to enzymes and their effects can be reversed by removing the inhibitor. Competitive reversible inhibitors bind to the active site, while non-competitive inhibitors bind elsewhere. Irreversible inhibitors covalently bond to enzymes and inactivate them. Allosteric inhibition involves inhibitors binding to allosteric sites which causes a change in the active site configuration.

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0% found this document useful (0 votes)
36 views25 pages

Enzyme Inhibition: Types and Definitions

Enzyme inhibition is a regulatory mechanism in biochemistry where inhibitors decrease the catalytic activity of enzymes. There are several types of inhibition including reversible, irreversible, and allosteric inhibition. Reversible inhibitors noncovalently bind to enzymes and their effects can be reversed by removing the inhibitor. Competitive reversible inhibitors bind to the active site, while non-competitive inhibitors bind elsewhere. Irreversible inhibitors covalently bond to enzymes and inactivate them. Allosteric inhibition involves inhibitors binding to allosteric sites which causes a change in the active site configuration.

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mehahe2105
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Enzyme inhibition

A regulatory mechanism in biochemistry

Ismail yasin bham.


231008
DEFINITION

Enzyme inhibitors are substances which bring about a


decrease in catalytic activity of the enzyme
Inhibitors may be organic or inorganic in nature
CLASSIFICATIONS

1. Reversible
2. Irreversible
3. Allosteric
REVERSIBLE
Inhibitors binds noncovalently with enzyme and the inhibition can be reversed if the
Inhibitor is removed

i . Competitive
ii . Non-competitive
COMPETITIVE INHIBITION
The inhibitor structurally resembles the substrate

The inhibitor binds at the active site of the enzyme instead of the substrate that
normally would, hence instead of an E-S complex, an E-I complex is formed

This inhibition can be overcome by a higher substrate concentration

No catalysis takes place.

Vmax remains the same, but Km is increased


COMPETITIVE
Examples

Allopurinol is the competitive inhibitor for the enzyme Xanthine oxidase.

Mellonate is a competitive inhibitor for succinate dehydrogenase.


NON COMPETITIVE
The inhibitor binds at a site other than the active site on the enzyme surface.

Inhibitor is not structurally similar to substrate

The enzyme-inhibitor complex can still bind with the substrate , but its efficiency
at transforming substrate to product is decreased

Vmax is lowered and Km is unchanged


NON COMPETITIVE
Examples
Fluoride inhibits glycolytic enzyme enolase

Cyanide inhibits cytochrome oxidase


IRREVERSIBLE
Inhibitors bond covalently with the Enzymes and inactivate them.

Usually toxic or poisonous substances

Once an enzyme is inhibited this way, it remains inactive until new enzyme
molecules are produced
SUICIDE INHIBITION

This is a special type of irreversible inhibition

An inhibitor binds to an enzyme, the inhibitor is then converted to a more potent


form by action of the enzyme, this irreversibly binds the enzyme and inhibitor

The reason this is referred to as suicidial is because the enzyme itself produces
the effective inhibitor which will inactivate said enzyme
EXAMPLE
Allopurinol gets oxidized by xanthine oxidase to form alloxanthine , a more potent
inhibitor of xanthine

The bacterial action of Penicillin is based on suicide inhibition of transpeptidase

Anti inflammatory action of Aspirin is also based on suicide inhibition of


cyclooxygenase by aspirin
ALLOSTERIC INHIBITION
All enzymes have one active site, some have an ‘allosteric’ site in addition to the
active site, where a modifier can bind

This modifier can either enhance or inhibit enzyme activity

Partially reversible

Km is usually increased, Vm in reduced

When inhibitor binds, the configuration of the active site is changed so substrate
cannot bind properly
ALLOSTERIC
EXAMPLE
FEEDBACK INHIBITION
The first step of a process is inhibited by the final product

This is a special type of allosteric inhibition

End product of a metabolic reaction produced in excess inhibits the first enzyme in
the sequence

Prevents build up of intermediates


Example
Production of ATP

Production of cholesterol
THANK YOU

AWEAH

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