As discussed during the lecture, the enzyme HIV-1 reversetranscriptae (HIV-RT) plays a significant role for the HIV virusand is an important drug target. Assume a concentration[E] of 2.00 µM (i.e. 2.00 x 10-6 mol/l) forHIV-RT. Two potential drug molecules, D1 andD2, were identified, which form stablecomplexes with the HIV-RT.
The dissociation constant of the complex ED1formed by HIV-RT and the drug D1 is 1.00 nM(i.e. 1.00 x 10-9 mol/l). The dissociation constant ofthe complex ED2 formed by HIV-RT and the drugD2 is 100 nM (i.e. 1.00 x 10-7mol/l).
1) Compute the difference in binding free energy (at aphysiological temperature T=310 K) for the complexes. Provide thedifference as a positive numerical expression with threesignificant figures in kJ/mol.
2) Divide the difference between the binding free energies ofthe ED1 and ED2 complexesby the thermal energy (at the physiological temperature). Provide anumerical expression with 3 significant figures.
3)
Compute the total concentration of[D1]tot that is needed to bind 90%of the HIV-RT at the given concentration[E]tot. Provide your answer as a numericalexpression with 3 significant figures in the unit mol/l.
You do NOT have to consider competition betwwen the drugsD1 and D2! They areadministered separately.
4)
Compute the total concentration of[D1]tot that is needed to bind 99%of the HIV-RT at the given concentration[E]tot. Provide your answer as a numericalexpression with 3 significant figures in the unit mol/l.
You do NOT have to consider competition betwwen the drugsD1 and D2! They areadministered separately.
5)
Compute the total concentration of[D2]tot that is needed to bind 90%of the HIV-RT at the given concentration[E]tot. Provide your answer as a numericalexpression with 3 significant figures in the unit mol/l.
You do NOT have to consider competition betwwen the drugsD1 and D2! They areadministered separately.
6)
Compute the total concentration of[D2]tot that is needed to bind 99%of the HIV-RT at the given concentration[E]tot. Provide your answer as a numericalexpression with 3 significant figures in the unit mol/l.
You do NOT have to consider competition betwwen the drugsD1 and D2! They areadministered separately.
