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enzymes are subject to inhibition ( enzyme inhibition)
pharmaceutical importance of enzyme inhibition study
enzyme inhibitors are molecular agents that interfere with catalysis, slowing or halting enzymatic reaction the most important pharmaceutical agents known.
example : aspirin → prostaglandin inhibitor → antiinflamation
anticancer agents → dna, rna, protein synthesis inhibitor (enzyme inhibitor)
classification
1) reversible inhibition
: competitive inhibition uncompetitive inhibition mixed inhibition
2) irreversible inhibition
1 enzyme inhibition
pharmaceutical importance of enzyme inhibition study
enzyme inhibitors are molecular agents that interfere with catalysis, slowing or halting enzymatic reaction the most important pharmaceutical agents known.
example : aspirin → prostaglandin inhibitor → anti-inflammation
anticancer agents → dna, rna, protein synthesis inhibitor (enzyme inhibitor)
classification
reversible inhibition : competitive inhibition
uncompetitive inhibition mixed inhibition irreversible inhibition to describe inhibition: ki
definition: ki (analogous to km) is the concentration of inhibitor at which it occupies half of the sites on the enzyme
it is conceptually equivalent to the dissociation constant of the enzyme, or enzyme-substrate complex, and the inhibitor
measure km and vmax in presence of i, get apparent
values… a.reversible inhibition same binding site 4 competitive inhibition
i binds to the same site as s, but can be competed away by adding more substrate, so
vmax is not affected
apparent km (km) will increase with inhibitor concentration.
vo vmax [s] km [s] 1 [i]/ki 5 competitive inhibition
i binds to the same site as s, but can be competed away by adding more substrate, so
vmax is not affected
apparent km (km) will increase with inhibitor concentration.
vo vmax [s] km [s] 1 [i]/ki 6 noncompetitive inhibition
since noncompetitive inhibitors do not interfere in the binding of the substrate (the dissociation constant of es and esi have the same value ks) (이하 생략)
