Ligand-binding kinetics

 

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Ligand-Binding Kinetics

A receptor switches between unbound and bound states. At the single-molecule level this looks like stochastic binding and unbinding.
At the population level it becomes a smooth occupancy curve. Change ligand concentration, kon, and koff to connect molecular events to ensemble behavior.






kon[L]
1.00

KD = koff/kon
2.50

Predicted occupancy θeq
0.67

Measured occupancy
0.67

Relaxation time τ
0.67 s

Single Receptor and Occupancy Trace

Ensemble Occupancy

Binding Curve and Current Operating Point

Main ideas
For a single receptor, binding looks noisy and intermittent. For many receptors, the same process averages into a smooth occupancy curve.
The equilibrium occupancy is
\(\theta_{eq} = \frac{[L]}{[L] + K_D}\), where \(K_D = k_{off}/k_{on}\).
The approach to equilibrium happens on a timescale \(\tau \approx 1/(k_{on}[L] + k_{off})\).