Enzyme Inhibition
(Competitive Inhibition)



  Presented by: Swapnil Agarwal
    Haren Patel, Vikshit Patel,
 Alok Priyadarshi, Purnima Singh,
   Parth Bhatt, Lakshesh Jadav
Enzyme – Enzyme – Enzyme!!!!

               What is it
                ????




                       Lets see……
Inhibitors
• Inhibitors are chemicals that reduce the rate
  of enzymic reactions
• The are usually specific and they work at low
  concentrations
• They block the enzyme but they do not usually
  destroy it
• Many drugs and poisons are inhibitors of
  enzymes in the nervous system
Enzyme Inhibitors
Enzyme inhibitors are molecules that reduce
the catalytic activity of enzymes. Reducing of
effective enzymatic activity or complete
blocking of enzyme may cause either
complete death of cell either modifications in
the pathways.

Appln: Drugs with cause complete inactivation
of enzymes from essential pathways will cause
cell death and therefore such drugs can be used
as an antibiotics.
Example:
Classification:
• Basis of Reversibility:
  – Reversible
  – Irreservisible


• Basis of Competitiveness:
  – Competitive
  – Un Competitive
  – Mixed
Basis of Reversibility:
• Reversible
• Reversible inhibitors bind to enzyme with only non
  covalent interactions.
• Reversible inhibitors do not perform any chemical
  changes in enzyme or themselves and they are in
  dynamic equilibrium with solution and can be removed
  from enzyme completely by reducing inhibitor
  concentration in solution.
• Reversible inhibition is often used as a self-regulated
  process in living cells, when the substrate or product of
  some enzymes acts as inhibitors for other enzymes.
Basis of Reversibility:
• Irreversible
• Irreversible inhibitors binds to enzyme via covalent
  bonds and prevent enzyme from further performing of
  catalytic acts.
• It is necessary to understand, that irreversible
  inhibitors act on some selected group of enzymes, with
  no effect on other enzymes and proteins.
• According to this classification it is impossible to
  consider chemical or physical agents which inactivate
  all enzymes and protein as an inhibitors.
Comparison:
Reversible                Irreversible
Binds via non covalent    Binds via covalent
interactions              interactions
Do not perform any        Inhibitor binds to the
chemical changes          substrate and prevent
                          catalytic activity of
                          enzymes.
Can be reversed, as there Irreversibility due to strong
is no bonding between the covalent bonding.
inhibitor and substrate.
Basis of competitiveness:
• Competitive Inhibition
  –As the name implies, compete with the
   substrate for active site of the enzyme.
  –Inhibitor is similar to natural
   substrates.
  –Most commonly occurred process.
Competitive – Uncompetitive!!!

                What is it
                 ????




                        Lets see……
Inhibition Kinetics:




Rate Law:

rp = kcat (E .S)
Rearranging:
Total Enzyme:
Lineweaver-Burk Plot
Misc:
• Video
• Allosteric Binding
•Case Study
Questions..??

Enzyme inhibition ppt final

  • 1.
    Enzyme Inhibition (Competitive Inhibition) Presented by: Swapnil Agarwal Haren Patel, Vikshit Patel, Alok Priyadarshi, Purnima Singh, Parth Bhatt, Lakshesh Jadav
  • 2.
    Enzyme – Enzyme– Enzyme!!!! What is it ???? Lets see……
  • 3.
    Inhibitors • Inhibitors arechemicals that reduce the rate of enzymic reactions • The are usually specific and they work at low concentrations • They block the enzyme but they do not usually destroy it • Many drugs and poisons are inhibitors of enzymes in the nervous system
  • 4.
    Enzyme Inhibitors Enzyme inhibitorsare molecules that reduce the catalytic activity of enzymes. Reducing of effective enzymatic activity or complete blocking of enzyme may cause either complete death of cell either modifications in the pathways. Appln: Drugs with cause complete inactivation of enzymes from essential pathways will cause cell death and therefore such drugs can be used as an antibiotics.
  • 5.
  • 6.
    Classification: • Basis ofReversibility: – Reversible – Irreservisible • Basis of Competitiveness: – Competitive – Un Competitive – Mixed
  • 7.
    Basis of Reversibility: •Reversible • Reversible inhibitors bind to enzyme with only non covalent interactions. • Reversible inhibitors do not perform any chemical changes in enzyme or themselves and they are in dynamic equilibrium with solution and can be removed from enzyme completely by reducing inhibitor concentration in solution. • Reversible inhibition is often used as a self-regulated process in living cells, when the substrate or product of some enzymes acts as inhibitors for other enzymes.
  • 8.
    Basis of Reversibility: •Irreversible • Irreversible inhibitors binds to enzyme via covalent bonds and prevent enzyme from further performing of catalytic acts. • It is necessary to understand, that irreversible inhibitors act on some selected group of enzymes, with no effect on other enzymes and proteins. • According to this classification it is impossible to consider chemical or physical agents which inactivate all enzymes and protein as an inhibitors.
  • 9.
    Comparison: Reversible Irreversible Binds via non covalent Binds via covalent interactions interactions Do not perform any Inhibitor binds to the chemical changes substrate and prevent catalytic activity of enzymes. Can be reversed, as there Irreversibility due to strong is no bonding between the covalent bonding. inhibitor and substrate.
  • 10.
    Basis of competitiveness: •Competitive Inhibition –As the name implies, compete with the substrate for active site of the enzyme. –Inhibitor is similar to natural substrates. –Most commonly occurred process.
  • 12.
    Competitive – Uncompetitive!!! What is it ???? Lets see……
  • 13.
  • 14.
  • 16.
  • 19.
  • 20.
    Misc: • Video • AllostericBinding •Case Study
  • 21.