05EnzymesInhibitionModePotencyDetermine

05EnzymesInhibitionModePotencyDetermine - Competitive...

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1 Competitive Inhibition E + S ES E + P + I EI k 1 k -1 k 2 K I V max [S] K m (1 + ) + [S] v = [ I ] K I or K i K i You expect TS analog inhibitors to be competitive inhibitors. So how would you tell?
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2 0.00 0.05 0.10 0.15 0.20 0.25 0.30 0.35 0.40 0.45 0.00 1.00 2.00 3.00 4.00 5.00 6.00 7.00 8.00 9.00 velocity [ S ] [ I ] = 0 [ I ] = 1 [ I ] = 2 Competitive inhibitors alter K m,eff but do not change V max . Competitive Inhibition
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3 A General Approach to Deriving Enzyme Kinetics, v=k i (ES) Use equilibrium or PSSA assumption to define all enzyme-modulator complexes Substitute into enzyme mass balance to find E=f(ES,E o ) Substitute E=f(ES,E o ) (or similar) into equilibrium/PSSA expression defining substrate binding Solve for ES Substitute into rate expression, simplify
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4 How to get from arrows to equation Assuming Rapid Equilibrium [] ES k v 2 = Rate expression ] [ ] ][ [ ES S E K m = ] [ ] ][ [ EI I E K I = Equilibrium expressions Enzyme Mass Balance [E 0 ] = [E] + [ES] + [EI] Get rid of E and EI V max [S] K m (1 + ) + [S] v = [ I ] K I [ E 0 ] [S] K m (1 + ) + [S] [ ES ] = [ I ] K I
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5 How to get from arrows to equation Assuming Pseudo Steady State [] ES k v 2 = Rate expression ] [ ] ][ [ EI I E K I = Equilibrium expressions Enzyme Mass Balance [E 0 ] = [E] + [ES] + [EI] Get rid of E and EI V max [S] K m (1 + ) + [S] v = [ I ] K I [ E 0 ] [S] K m (1 + ) + [S] [ ES ] = [ I ] K I Steady-State
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6 0.00 0.05 0.10 0.15 0.20 0.25 0.30 0.35 0.40 0.45 0.00 1.00 2.00 3.00 4.00 5.00 6.00 7.00 8.00 9.00 velocity [ S ] [ I ] = 0 [ I ] = 1
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05EnzymesInhibitionModePotencyDetermine - Competitive...

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