1)Drug X binds to two sites (S-1 & S-2 where the former is associated with the t

Question

1)Drug X binds to two sites (S-1 & S-2 where the former is associated with the therapeutic effect and the latter with an adverse effect) with a 10-fold difference in affinity (i.e., KD at S-2 = 10(KD at S-1). At a concentration of Drug X that binds to 80% of the higher affinity S-1 sites, how much binding (i.e., what fractional occupancy) will occur at S-2? 2)How much of a difference in KD is needed for 90% occupancy at a high affinity (i.e., therapeutic site) site and 5% occupancy at the low affinity site (i.e., site causing toxicity)?

Explanation / Answer

Part a: binding at site b= 80 * 1 / 10 = 8% Part b: 90 / 5 = 18. difference in Dissociation constant = 18 times for s -1 and s-2

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