Signal Transduction and Drug Action

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Questions and Answers

What is a consequence of the permanent activation of HER2 in breast cancer?

  • Inhibition of cell growth
  • Increased apoptosis
  • Unregulated cell division (correct)
  • Decreased cell division

How does Lapatinib affect HER2 in breast cancer treatment?

  • It permanently activates the HER2 receptor
  • It inhibits phosphorylation of the HER2 receptor (correct)
  • It enhances receptor auto-phosphorylation
  • It blocks HER2 gene expression

What percentage of human breast cancers is associated with the permanent activation of HER2?

  • 10 percent
  • 20 percent
  • 40 percent
  • 30 percent (correct)

What is the effect of Lapatinib on tumor growth in breast cancer patients?

<p>Reduces tumor growth by 50 percent (A)</p> Signup and view all the answers

What is the mechanism by which HER2 contributes to breast cancer progression?

<p>By enabling rapid cell division (C)</p> Signup and view all the answers

What is the main function of the drugs that bind to the GABAA receptor–chloride channel complex?

<p>To facilitate the opening of channels in response to GABA. (B)</p> Signup and view all the answers

Which ion channels are classified as voltage-gated according to the content?

<p>Sodium (Na+), potassium (K+), calcium (Ca2+), and chloride (Cl–). (D)</p> Signup and view all the answers

What differentiates the action of drugs that bind to the GABAA receptor?

<p>They bind to a distinct region not involved in neurotransmitter reuptake. (B)</p> Signup and view all the answers

Which of the following statements about voltage-gated channels is correct?

<p>They can be activated or inactivated by changes in voltage across the membrane. (B)</p> Signup and view all the answers

How do the drugs that interact with the GABAA receptor affect GABA's physiological role?

<p>They enhance the efficacy of GABA by promoting channel opening. (D)</p> Signup and view all the answers

What is the primary role of signal transduction cascades in pharmacology?

<p>To amplify the signal of the drug. (C)</p> Signup and view all the answers

How do intracellular signaling pathways affect cellular responses?

<p>They produce multiple intracellular signals for one receptor. (B)</p> Signup and view all the answers

Which statement accurately describes the function of cascades in relation to receptor binding?

<p>Cascades amplify the signal from a single receptor binding. (A)</p> Signup and view all the answers

What effect do signal transduction cascades have on drug effectiveness?

<p>They can enhance the effectiveness by producing multiple signals. (B)</p> Signup and view all the answers

What is the relationship between receptor binding and the number of signals produced by cascades?

<p>One receptor binding leads to multiple signals produced. (B)</p> Signup and view all the answers

What is the primary function of nuclear receptors?

<p>Serve as transcription factors regulating gene expression. (B)</p> Signup and view all the answers

Which of the following biological processes are nuclear receptors involved in regulating?

<p>Cell proliferation, metabolism, immunity, and development. (A)</p> Signup and view all the answers

Nuclear receptors can be described as which of the following?

<p>Transcription factors involved in gene regulation. (B)</p> Signup and view all the answers

In which domain of biology do nuclear receptors primarily operate?

<p>Cell biology regulating genetic transcription mechanisms. (D)</p> Signup and view all the answers

What is one of the consequences of nuclear receptor activation?

<p>Altered expression of target genes leading to changes in cell function. (D)</p> Signup and view all the answers

What role does the activated G-protein serve in cellular signaling?

<p>It interacts with either an ion channel or an enzyme in the membrane. (A)</p> Signup and view all the answers

What is a defining characteristic of the family of transmembrane receptors mentioned?

<p>They consist of seven transmembrane domains. (C)</p> Signup and view all the answers

Why is the specific extracellular domain important for G-protein coupled receptors?

<p>It ensures the receptor can bind to distinct ligands. (A)</p> Signup and view all the answers

Which statement best describes the G-protein-binding site of the receptors?

<p>It varies between different receptor types. (B)</p> Signup and view all the answers

What is the primary function of the seven transmembrane domains in these receptors?

<p>They anchor the receptor in the cell membrane. (D)</p> Signup and view all the answers

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Study Notes

Signal Transduction Cascades

  • Cascades amplify the signal of a drug.
  • They produce multiple intracellular signals for every receptor bound.
  • These cascades are also called intracellular signalling pathways.

GABA Receptor

  • Drugs that bind to these receptors facilitate the opening of the chloride channel by GABA.
  • This binding site is distinct from the GABA binding site.

Voltage-gated Channels

  • There are many isoforms of voltage-gated channels, such as sodium, potassium, calcium, and chloride.

G-protein Coupled Receptors (GPCRs)

  • These receptors are a large family of transmembrane receptors with seven transmembrane domains.
  • Each GPCR has a specific extracellular domain and G-protein binding site.
  • Upon activation, the G-protein interacts with either an ion channel or an enzyme in the membrane.

HER2 Receptor

  • In 30% of human breast cancers, the HER2 receptor is permanently activated, leading to unregulated cell division.
  • The drug lapatinib inhibits HER2 receptor tyrosine kinase auto-phosphorylation, reducing tumor growth by 50%.

Nuclear Receptors

  • These receptors are factors that regulate complex regulatory networks.
  • They play a role in important biological processes, including:
    • Cell proliferation
    • Metabolism
    • Immunity
    • Development

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