Signaling Across Biomembranes
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Questions and Answers

What role do secondary messengers play in signal transduction?

  • They inhibit the action of primary messengers.
  • They act as the main receptors for cellular ligands.
  • They transmit information further downstream. (correct)
  • They are responsible for the removal of local signals.

What is primarily responsible for phosphorylation in cellular signaling?

  • G protein-coupled receptors
  • Phosphatase family of enzymes
  • Ligand-gated ion channels
  • Kinase family of enzymes (correct)

What characterizes cell-surface receptors?

  • They can only bind to non-hydrophilic molecules.
  • They only respond to small molecular weight ligands.
  • They require crossing the plasma membrane to transmit signals.
  • They consist of multiple domains including an extracellular ligand-binding domain. (correct)

Which of the following processes can lead to the activation of cellular responses?

<p>Either phosphorylation or dephosphorylation depending on the context (D)</p> Signup and view all the answers

Which type of receptor is known to directly form ion channels upon ligand binding?

<p>Ligand-gated ion channels (D)</p> Signup and view all the answers

What is the primary mechanism by which cholera induces severe diarrhea in the intestinal epithelium?

<p>Increased cAMP leading to efflux of Cl and water (C)</p> Signup and view all the answers

Which type of receptor is primarily involved in regulating cell growth and metabolism through tyrosine kinase activity?

<p>Receptor Tyrosine Kinase (RTK) (A)</p> Signup and view all the answers

What triggers the dimerization of Receptor Tyrosine Kinases (RTKs)?

<p>Binding of a ligand such as insulin or growth factors (D)</p> Signup and view all the answers

In the context of Pertussis toxin, what is the outcome of its effect on the Gi subunit?

<p>Activation of adenylate cyclase (D)</p> Signup and view all the answers

Which type of receptor responds by autophosphorylating serine or threonine residues upon ligand binding?

<p>Receptor Serine/Threonine Kinase (B)</p> Signup and view all the answers

Which effect does the stimulation of influx of chloride through GABA receptor A achieve?

<p>Suppresses neuronal function (D)</p> Signup and view all the answers

How does the modulation of Gi proteins affect blood pressure in hypertension?

<p>It inhibits adenylate cyclase (A)</p> Signup and view all the answers

What is the primary action of drugs acting on β2 adrenergic receptors?

<p>Increase cyclic AMP production (A)</p> Signup and view all the answers

What is the role of Gq proteins in response to α1 adrenergic receptor activation?

<p>To activate phospholipase C (A)</p> Signup and view all the answers

Drugs targeting enzyme-linked receptors are primarily used for which purpose?

<p>To control autoimmunity and inflammation (D)</p> Signup and view all the answers

What is the primary consequence of gene mutations in chloride channels related to Cystic Fibrosis?

<p>High concentrations of Na+ and Cl– in sweat and viscous mucus (C)</p> Signup and view all the answers

Which characteristic is shared by all G protein-coupled receptors?

<p>They contain a heterotrimeric G protein in an inactive state (C)</p> Signup and view all the answers

What is the function of the Gs protein subunit in G protein signaling?

<p>Stimulates adenylate cyclase and the cyclic AMP pathway (C)</p> Signup and view all the answers

What results from the action of cholera toxin on G proteins?

<p>Sustained activation of the α subunit of Gs (C)</p> Signup and view all the answers

What is a characteristic of ligand-gated ion channels?

<p>They can also close in response to ligand binding (D)</p> Signup and view all the answers

Flashcards

Secondary Messengers

Molecules that transmit signals within a cell, often triggered by external signals.

Signal Transduction Cascade

A series of biochemical reactions inside a cell that convert an external signal into a cellular response.

Phosphorylation

The addition of a phosphate group to a protein, often to activate or deactivate it.

Ligand-Gated Ion Channels

Membrane proteins that open or close ion channels in response to a signal molecule (ligand).

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Cell-Surface Receptors

Proteins embedded in the cell membrane that bind to signaling molecules (ligands) outside the cell, initiating a cellular response.

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Cystic Fibrosis

A genetic disorder caused by mutations in chloride channels, leading to thick mucus buildup in the lungs, pancreas, and other organs.

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G Protein-Coupled Receptors (GPCRs)

A large family of cell surface receptors that use G proteins to transmit signals inside the cell. Changes occur from inactive to active state by binding of ligands.

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G protein

A protein that acts as a molecular switch inside cells, relaying signals from G protein-coupled receptors. It's inactive when bound to GDP, active when bound to GTP.

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Cholera toxin

A bacterial toxin that modifies a G protein (Gs) keeping it permanently activated, leading to excessive fluid loss.

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Cholera's mechanism of diarrhea

Cholera increases cAMP in intestinal cells, causing a large release of Cl- and water into the gut, leading to severe diarrhea.

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Pertussis toxin effect on airway epithelium

Pertussis toxin activates a subunit of Gi in airway cells, inhibiting the exchange of GDP for GTP, thus increasing cAMP, and causing fluid imbalance and airway congestion.

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Enzyme-linked receptors

Receptors for growth factors, cytokines, and hormones. They have extracellular ligand-binding domains, transmembrane helices, and intracellular effector domains with enzyme activity.

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Receptor Tyrosine Kinase (RTK) activation

RTKs are single-unit receptors that dimerize upon ligand binding, causing tyrosine kinase activation. This leads to autophosphorylation and downstream signaling via proteins like RAS.

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RTK downstream signaling

RAS, a small G-protein, is a key downstream signal of RTK and plays a role in regulating cell growth and proliferation.

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Nicotinic Receptor Modulation

Drugs can inhibit the flow of sodium (Na+) into and potassium (K+) out of muscle cells by binding to nicotinic receptors. This helps muscle relaxation during surgery, as seen with anesthetics.

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GABA Receptor Modulation

Drugs can stimulate the influx of chloride (Cl-) into neurons by binding to GABA receptors. This suppresses neuronal activity, helping to treat convulsions and induce sleep.

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Gs Protein Activation

Drugs can activate Gs proteins linked to beta-2 adrenergic receptors, leading to increased cAMP production and activation of protein kinase A (PKA). This causes bronchodilation, helpful in bronchial asthma.

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Gi Protein Inhibition

Drugs can inhibit Gi proteins linked to alpha-2 adrenergic receptors, reducing cAMP production and PKA activity. This lowers blood pressure, useful in hypertension.

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Gq Protein Activation

Drugs can activate Gq proteins linked to alpha-1 adrenergic receptors, leading to increased IP3 and DAG production, and PKA activation. This raises blood pressure, helpful during surgery to counteract anesthesia-induced hypotension.

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Study Notes

Signaling Across Biomembranes

  • Signals from cells are mostly chemicals released into the extracellular fluid
  • Signals can be transported to distant targets (endocrine), adjacent cells (paracrine), or the same cell (autocrine)
  • Signaling conveys information to target cells, influencing processes like metabolism, gene expression, cell division, and differentiation
  • Cell signaling has three stages: reception, transduction, and response
    • Reception: A cell recognizes a signal molecule (ligand) by a specific protein (receptor) on its surface or within the cytosol or nucleus
    • Transduction: The binding of ligand to receptor initiates a cascade of events that amplify or integrate the signal
    • Response: The final step in signal transduction that produces a cellular response, such as contraction, secretion, or metabolic reaction.
  • Membrane receptors bind ligands outside the cell without crossing the plasma membrane. These include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked receptors.
  • Ligand-gated ion channels allow ions to cross the membrane in response to ligand binding, rapidly changing cellular response.
  • G protein-coupled receptors (GPCRs) are a large receptor family that use G-proteins to transmit signals inside the cell.
  • Enzyme-linked receptors transmit signals through intracellular enzymes, like receptor tyrosine kinases (RTKs). These are involved in many cell growth and development processes.
  • Receptor proteins can be categorized by their structure and methods of signaling.
  • Phosphorylation/dephosphorylation regulate proteins involved in signal transduction.

Drug Modulation of Cell Signaling

  • Drugs can modulate cell signaling through various mechanisms, including acting on receptors, enzymes, or ion channels.
  • Drugs can act outside the cell membrane, on cell surface receptors, and on intracellular receptors.
  • Drugs can modulate diverse cellular functions by binding in place of ligands, altering ion flow in ion channels, affecting intracellular second messengers, inhibiting/activating downstream signaling pathways, or directly regulating the receptor expression.
  • Drugs can bind to receptors:
    • As agonists (mimicking natural ligands), triggering a cellular response
    • As antagonists (blocking natural ligands), preventing a cellular response
    • Drugs can also be inverse agonists (reverse the signaling).
  • A graded dose-response curve plots the relationship between drug concentration and response.
  • Drugs can be categorized as competitive reversible or competitive irreversible antagonists based on their binding.
  • Drugs can also be non-competitive or allosteric antagonists that bind to a different site on the receptor.
  • Important considerations about drug affinity and potency in targeting biological pathways are required.

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Description

Explore the intricate process of cell signaling, which involves the interaction of signals and receptors to influence cellular functions. This quiz covers the three stages of cell signaling: reception, transduction, and response, along with types of signaling pathways. Understand how these processes affect metabolism, gene expression, and more.

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