can someone explain how the drug reacts better than the protein? i feel like the

Question

can someone explain how the drug reacts better than the protein? i feel like the Kd for the protein is smaller, meaning that the affinity is lower so it binds better?

8. (10 points) A new drug was compared with a protein isolated that inhibits HIV interaction with a specific receptor. You collected the following data. Which molecule interacts (drug or protein) the best with the receptor and why do you think so based on the data? Provide an estimate of the Kd for the interaction, in each case. Write a chemical equilibrium equation that describes the control Ke value 1.2 L 0.8 0.6 0.4 0.2 Contrel hProtein present -Drug Present 0 5 10 15 20 25 Concentration of HIV (nM) Drug clearly interacts better with the receptor as a higher concentration of HIV is required to reach saturation of receptors (1.5 points) Kd of the control appears to be around 1 nM. It is around 3 nM for protein present and around 10 nM for drug present (2.5 points for each) - The Receptor + HIV HIV-Receptor( 1 point)

Explanation / Answer

Answer:

In case of control, HIV binds to receptor at a very low concentration and the saturation occurs early.

In presence of protein, the fractional occupancy is lower and reaches saturation at around 20nM concentration of HIV.

In presence of inhibitor, the fractional occupancy reduces further, more concentration of HIV is required to reach 50% fractional occupancy as compared to control and protein alone.

Kd (equilibrium dissociation constant) is the inverse of the drug affinity to the binding site. That means a lower Kd value indicates higher affinity of binding and conversely a higher Kd value indicates lower affinity of binding.

Since Kd value in presence of inhibitor is the highest (10nM), therefore in presence of drug the binding affinity of HIV to receptor is reduced as compared to in presence of protein alone.

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