WK 2:  Receptors and Enzymes as Drug Targets
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Questions and Answers

What is the primary mechanism by which drugs interact with their targets?

  • Through intermolecular repulsion
  • Through ionic interactions
  • Through covalent bonds
  • Through intermolecular bonds (correct)

What is the term for specific regions within the binding site involved in binding interactions?

  • Active site
  • Binding site
  • Receptor site
  • Binding regions (correct)

What is the term for molecules that bind to receptors and produce a response?

  • Antagonists
  • Agonists (correct)
  • Activators
  • Inhibitors

What is the term for molecules that bind to enzymes, reducing their activity?

<p>Competitive inhibitors (A)</p> Signup and view all the answers

What is the 'lock and key' hypothesis related to?

<p>Receptor-ligand interactions (A)</p> Signup and view all the answers

What is the term for molecules that bind to receptors, reducing their response?

<p>Antagonists (A)</p> Signup and view all the answers

What is the primary function of receptors in cellular function?

<p>To initiate changes in cellular function (B)</p> Signup and view all the answers

What is a characteristic of receptors in relation to drugs?

<p>Many drugs can bind to multiple receptors (C)</p> Signup and view all the answers

What is the term for the process by which a receptor changes its structure in response to binding to a drug?

<p>Induced-fit hypothesis (A)</p> Signup and view all the answers

Which of the following is NOT a type of protein target for drugs?

<p>DNA (C)</p> Signup and view all the answers

What is the role of enzymes in cellular function?

<p>To convert substrates into products (D)</p> Signup and view all the answers

What is the purpose of molecular modelling in drug design?

<p>To simulate drug binding and interactions (B)</p> Signup and view all the answers

What is the primary function of an antagonist?

<p>To block the action of an agonist (A)</p> Signup and view all the answers

What is the difference between competitive and non-competitive antagonists?

<p>Competitive antagonists bind to the ligand binding site, while non-competitive antagonists bind to a different site (B)</p> Signup and view all the answers

What is the effect of an irreversible antagonist on a receptor?

<p>It forms a covalent bond to the active site (C)</p> Signup and view all the answers

What is the function of the nicotinic acetylcholine receptor?

<p>To transmit signals across the neuromuscular junction (A)</p> Signup and view all the answers

What is the effect of Tubocurarine on the nicotinic acetylcholine receptor?

<p>It acts as an antagonist, blocking muscle contraction (D)</p> Signup and view all the answers

What is the definition of a ligand?

<p>A molecule that binds to a receptor, eliciting a response (C)</p> Signup and view all the answers

Which type of adrenergic receptors is found in adipose tissue?

<p>b1 and b3 (C)</p> Signup and view all the answers

What is the effect of agonists on receptors?

<p>They bind and activate receptors (B)</p> Signup and view all the answers

What is the term for compounds that bind to receptors but do not activate them?

<p>Antagonists (D)</p> Signup and view all the answers

Which of the following is a characteristic of agonists?

<p>They have a structural similarity to endogenous ligands (C)</p> Signup and view all the answers

What is the effect of binding of an agonist to a receptor?

<p>An increase in the downstream response (C)</p> Signup and view all the answers

What is the role of endogenous agonists in the body?

<p>They are naturally occurring compounds that bind to receptors (D)</p> Signup and view all the answers

What is the mechanism of competitive inhibition in enzymes?

<p>A drug acts as a substrate analogue to reversibly block the enzyme's active site (C)</p> Signup and view all the answers

What is the effect of non-competitive inhibition on an enzyme?

<p>The overall shape of the enzyme is altered (B)</p> Signup and view all the answers

What type of inhibition can be both competitive and non-competitive?

<p>Irreversible inhibition (A)</p> Signup and view all the answers

What is the role of coenzymes in enzyme-catalyzed reactions?

<p>To convert the substrate into product (D)</p> Signup and view all the answers

What is the result of blocking the enzyme HMG-CoA reductase?

<p>Decreased synthesis of cholesterol (A)</p> Signup and view all the answers

What is the term for drugs that bind to enzymes and reduce their activity?

<p>Inhibitors (B)</p> Signup and view all the answers

Flashcards

Drug interaction mechanism

Drugs interact with their targets primarily through intermolecular bonds.

Binding regions

Specific parts of a binding site where molecules attach.

Agonist

A molecule that binds to receptors and starts a response.

Competitive inhibitor

A molecule that binds to an enzyme, reducing its activity by blocking the active site.

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Lock-and-key hypothesis

The idea that receptors and ligands match up perfectly.

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Antagonist

Binds to receptors and reduces their response.

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Receptor function

Receptors initiate changes in cells.

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Drug receptor binding

Many drugs can bind to more than one type of receptor.

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Induced-fit hypothesis

The receptor changes shape when a drug binds.

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Non-protein drug target

DNA is not a protein target for drugs.

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Enzyme function

Enzymes convert substrates into products.

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Molecular modeling

Simulates drug interactions to design new drugs.

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Antagonist function

Antagonists block the action of agonists.

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Competitive vs. Non-competitive antagonists

Competitive - bind to the ligand binding site. Non-competitive - bind to a different site.

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Irreversible antagonist

Forms a covalent bond with the active site.

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Nicotinic acetylcholine receptor function

Transmits signals across neuromuscular junctions.

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Tubocurarine effect

Blocks muscle contraction by acting as an antagonist.

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Ligand

A molecule that binds to a receptor, causing a response.

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Adipose tissue receptor type

b1 and b3 adrenergic receptor types are found in adipose tissue.

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Agonist effect on receptors

Binding and activation of receptors by agonists.

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Antagonist structural nature

Compounds that bind to receptors but do not activate them.

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Agonists property

Agonists structurally similar to endogenous ligands.

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Agonist binding effect

Binding of an agonist increases the downstream response.

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Endogenous agonists

Naturally occurring compounds that bind to receptors.

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Competitive inhibition mechanism

Drugs act like substrate analogues to temporarily block enzyme active sites.

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Non-competitive inhibition effect

Alters the enzyme's overall shape, reducing activity.

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Irreversible inhibition

Can be both competitive and non-competitive.

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Coenzyme role

Essential for converting substrate to product in enzyme-catalyzed reactions.

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HMG-CoA reductase inhibition

Reduces cholesterol synthesis.

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Enzyme inhibitor

Drugs that bind to enzymes and reduce their activity.

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