Suppose that Protein J which is a hypothetical protein kinase receptor was determined to be related to the progression of cancer through its activation. It was also determined that the protein exists in the active and inactive forms. The said active form is highly similar to the Protein K's conformation. Ligands A, B, and C, which are lead inhibitor compounds, were optimized to inhibit Protein J. The affinities of the ligands are shown in the table. Kp values Active Protein J Inactive Protein J Protein K Ligand A 10 mM 20 nM 5 mM Ligand B 20 nM 10 mM 15 nM Ligand C 20 nM 15 nM 15 nM Question: Describe the relative binding affinities of Ligand A to Protein K and to the active and inactive forms of Protein J. Determine which will Ligand A bind with the highest, medium, and lowest affinity.

Biochemistry
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Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
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Chapter1: Biochemistry: An Evolving Science
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Suppose that Protein J which is a hypothetical protein kinase receptor was determined to
be related to the progression of cancer through its activation. It was also determined that the
protein exists in the active and inactive forms. The said active form is highly similar to the Protein
K's conformation. Ligands A, B, and C, which are lead inhibitor compounds, were optimized to
inhibit Protein J. The affinities of the ligands are shown in the table.
Kp values
Active Protein J
Inactive Protein J
Protein K
Ligand A
10 mM
20 nM
5 mM
Ligand B
20 nM
10 mM
15 nM
Ligand C
20 nM
15 nM
15 nM
Question:
Describe the relative binding affinities of Ligand A to Protein K and to the active and inactive forms of
Protein J. Determine which will Ligand A bind with the highest, medium, and lowest affinity.
Transcribed Image Text:Suppose that Protein J which is a hypothetical protein kinase receptor was determined to be related to the progression of cancer through its activation. It was also determined that the protein exists in the active and inactive forms. The said active form is highly similar to the Protein K's conformation. Ligands A, B, and C, which are lead inhibitor compounds, were optimized to inhibit Protein J. The affinities of the ligands are shown in the table. Kp values Active Protein J Inactive Protein J Protein K Ligand A 10 mM 20 nM 5 mM Ligand B 20 nM 10 mM 15 nM Ligand C 20 nM 15 nM 15 nM Question: Describe the relative binding affinities of Ligand A to Protein K and to the active and inactive forms of Protein J. Determine which will Ligand A bind with the highest, medium, and lowest affinity.
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