You are the lead scientist for a pharmaceutical company responsible for evaluating over 30,000 known compounds as potential drugs that inhibit a specific human enzyme that is often over-expressed in cancer cells. Your team has purified this phosphodiesterase and done initial assays to test for inhibition by all 30,000 compounds. You have asked your team to more fully test the two compounds that showed the strongest inhibition of the phosphodiesterase (both showed 50% inhibition of the phosphodiesterase at inhibitor concentrations of 1 g/ml. Below are the results for their enzyme assays of velocity (Velocity units are umoles of product formed per minute) of the reaction as a function of the substrate concentration. The Vice-President for Research in your company wants to know which compound to bring to clinical trial (Phase I trials run to several million dollars, so you get to choose only one). She needs the answer and a justification of your choice by Friday. [S] uM V unihib V inhib A V inhib B 1/S 1/V unihib 1/V A 1/V B 1 0.09 0.05 0.08 1.00 11.11 20.00 12.50 3 0.23 0.13 0.19 0.33 4.35 7.69 5.26 10 0.5 0.33 0.33 0.10 2.00 3.03 3.03 30 0.75 0.61 0.43 0.03 1.33 1.64 2.33 100 0.91 0.83 0.48 0.01 1.10 1.20 2.08 Your colleagues mentioned that the normal physiological range of the substrate phosphodiester in humans is 30-50 microM. Would you have chosen differently if the normal substrate concentration was below 1 microM?
You are the lead scientist for a pharmaceutical company responsible for evaluating over
30,000 known compounds as potential drugs that inhibit a specific human enzyme that is
often over-expressed in cancer cells. Your team has purified this phosphodiesterase and
done initial assays to test for inhibition by all 30,000 compounds. You have asked your
team to more fully test the two compounds that showed the strongest inhibition of the
phosphodiesterase (both showed 50% inhibition of the phosphodiesterase at inhibitor
concentrations of 1 g/ml. Below are the results for their enzyme assays of velocity
(Velocity units are umoles of product formed per minute) of the reaction as a function of
the substrate concentration. The Vice-President for Research in your company wants to
know which compound to bring to clinical trial (Phase I trials run to several million
dollars, so you get to choose only one). She needs the answer and a justification of your
choice by Friday.
[S] uM V unihib V inhib A V inhib B 1/S 1/V unihib 1/V A 1/V B
1 0.09 0.05 0.08 1.00 11.11 20.00 12.50
3 0.23 0.13 0.19 0.33 4.35 7.69 5.26
10 0.5 0.33 0.33 0.10 2.00 3.03 3.03
30 0.75 0.61 0.43 0.03 1.33 1.64 2.33
100 0.91 0.83 0.48 0.01 1.10 1.20 2.08
Your colleagues mentioned that the normal physiological range of the substrate
phosphodiester in humans is 30-50 microM. Would you have chosen differently if the normal
substrate concentration was below 1 microM?
Trending now
This is a popular solution!
Step by step
Solved in 3 steps with 2 images
