Which of the following features should an effective transition state analog inhi
ID: 561378 • Letter: W
Question
Which of the following features should an effective transition state analog inhibitor have (select all that apply)? (Hint: be sure you know what type of inhibitor transition state analogs are, and then identify which features enhance the behavior of that type of inhibitor.)
Interactions with the residues that stabilize the transition state (hint: this is not the same thing as actually binding to the transition state; again keep in mind the type of inhibitor)
The ability to covalently bond to an active site residue
The same overall charge as residues present in the active site
Being small enough that the substrate can also still bind to the enzyme
Interactions with the residues that stabilize the substrate
Interactions with the residues that stabilize the transition state (hint: this is not the same thing as actually binding to the transition state; again keep in mind the type of inhibitor)
The ability to covalently bond to an active site residue
The same overall charge as residues present in the active site
Being small enough that the substrate can also still bind to the enzyme
Interactions with the residues that stabilize the substrate
Explanation / Answer
First two feature are responsible for produce an effective transition state. If there are strong interactions with residues then that will produce more stable transition state.
If the inhibitor has ability to form covalent bonds with active site residue then also transition state will be more stabilized.
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