Typen medicijnen en drugtargets - Receptors as drug targets

6 important questions on Typen medicijnen en drugtargets - Receptors as drug targets

How should agonists bind?

Agonists should bind and leave quickly. The number of binding interactions is important for agonists.

How do antagonists tend to interact with receptors?

Antagonists tend to have stronger and/or more binding interactions, resulting in a different induced fit such that the receptor is not activated.
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What are the requirements of agonists?

-Must have the correct binding group.
-Binding groups must be correctly positioned to interact with complementary binding regions
-The drug must have the correct shape to fit the binding site
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What are groups called that prevent access to the binding site?

Steric shields

Do antagonists activate the receptor?

No, antagonists fail to produce the correct induced fit, so the receptor is not activated.

What is the consequence of an antagonist binding to a receptor?

The normal messenger is blocked from binding.

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