Signal Amplification in Signaling Pathways

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Questions and Answers

Which term describes the phenomenon where the number of activated participants in a signal transduction pathway increases at each step?

  • Signal amplification (correct)
  • GTPase activation
  • Amplification switch
  • Phosphorylation cascade

What type of proteins play important roles in intracellular signal transduction by being active when bound to GTP and inactive when bound to GDP?

  • Kinases
  • Adenylyl cyclases
  • Hormone receptors
  • GTPase switch proteins (correct)

Which proteins promote the exchange of GTP for GDP and activate GTPases?

  • Kinases
  • GTPase-activating proteins (GAPs)
  • Adenylyl cyclases
  • Guanine nucleotide-exchange factors (GEFs) (correct)

What do kinases use to phosphorylate amino acid sidechains in target proteins?

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

Which type of proteins stimulate the rate of GTP hydrolysis to GDP and inactivate GTPases?

<p>GTPase-activating proteins (GAPs) (A)</p> Signup and view all the answers

What is estimated to be the overall amplification associated with epinephrine signaling?

<p>~100-fold (B)</p> Signup and view all the answers

Which type of signaling pathways are often referred to as amplification cascades?

<p>Hormone signaling pathways (C)</p> Signup and view all the answers

What is the function of hormone-activated GPCRs in epinephrine signaling?

<p>Activate many adenylyl cyclases (B)</p> Signup and view all the answers

What is the role of an orthosteric ligand in GPCR signaling?

<p>It binds to an inactive GPCR to activate it (D)</p> Signup and view all the answers

How many distinct GPCRs have had their crystal structures solved so far?

<p>44 (D)</p> Signup and view all the answers

Which subfamily do all the four classes A–C, and F belong to?

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

What is the primary outcome of binding of a ligand to a GPCR?

<p>Activation of downstream effectors (A)</p> Signup and view all the answers

In GPCR signaling, what happens when a GPCR binds a G protein?

<p>The α chain dissociates from the b g complex and binds to its effector molecule (C)</p> Signup and view all the answers

What does IC PAM refer to in the context of GPCR crystal structures?

<p>Binding of a ligand to an inhibitor (A)</p> Signup and view all the answers

What is the function of a GPCR as a GEF?

<p>Allows binding of G protein by changing the conformation of the receptor (A)</p> Signup and view all the answers

What is the main outcome of ligand binding in G-protein receptor activation?

<p>Switching the α subunit to its activated state (A)</p> Signup and view all the answers

What is the primary role of bound GTP in G-protein receptor activation?

<p>Dissociation from the bg complex and binding to its effector molecule (B)</p> Signup and view all the answers

Which type of GPCR has seven transmembrane helices?

<p>Class A/Rhodopsin family GPCRs (D)</p> Signup and view all the answers

What type of ligands are shown as purple sticks in the representative structures?

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

What do the prenyl groups -3-methylbut-2-en-1-yl represent in the context of GPCR?

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

In which class of nonrhodopsin GPCRs is the representative structure A2A AR found?

<p>Nucleotide-like (D)</p> Signup and view all the answers

What differentiates class A/Rhodopsin family GPCRs from other classes?

<p>Presence of seven transmembrane helices (B)</p> Signup and view all the answers

What is the role of helix VIII in GPCRs?

<p>Runs parallel to the membrane near the C-terminus (A)</p> Signup and view all the answers

Which class of nonrhodopsin GPCR does the representative structure SMO belong to?

<p>Class F GPCRs (C)</p> Signup and view all the answers

What type of ligands are shown as blue stick models in the representative structures?

<p>Negative allosteric modulators (D)</p> Signup and view all the answers

What is the composition of class B GPCRs?

<p>CRF1, GCGR, GLP-1R, CTR (B)</p> Signup and view all the answers

What is the overall amplification associated with epinephrine signaling estimated to be?

<p>~10^8-fold (D)</p> Signup and view all the answers

What is the primary role of guanine nucleotide-exchange factors (GEFs) in intracellular signal transduction?

<p>Promote exchange of GTP for GDP and activate GTPases (A)</p> Signup and view all the answers

Which proteins play important roles in intracellular signal transduction by being active when bound to GTP and inactive when bound to GDP?

<p>GTPase switch proteins (A)</p> Signup and view all the answers

What is the function of GTPase-activating proteins (GAPs) in the regulation of signaling ON/OFF?

<p>Stimulate the rate of GTP hydrolysis to GDP and inactivate GTPases (B)</p> Signup and view all the answers

Which proteins use ATP to phosphorylate amino acid sidechains in target proteins?

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

Which type of G-protein coupled receptor (GPCR) family consists of hundreds of receptors and has a 7-transmembrane (7TM) structure in the membrane?

<p>Class A/Rhodopsin family (B)</p> Signup and view all the answers

Which type of ligand is represented by purple sticks in the representative structures of GPCRs?

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

What is the role of helix VIII in GPCRs?

<p>It is located near the crystallization techniques (B)</p> Signup and view all the answers

In GPCR signaling, what happens when a GPCR binds a G protein?

<p>The G protein releases GDP and binds to GTP (D)</p> Signup and view all the answers

What do the prenyl groups -3-methylbut-2-en-1-yl represent in the context of GPCR?

<p>They form part of the γ subunit prenylation (C)</p> Signup and view all the answers

What is the primary outcome of binding of a ligand to a GPCR?

<p>Conformational change in the receptor (D)</p> Signup and view all the answers

Which class of nonrhodopsin GPCR does the representative structure SMO belong to?

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

In which part of the cell membrane are nonrhodopsin GPCRs typically located?

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

What is the primary challenge in elucidating GPCR structures?

<p>Allosteric binding sites (B)</p> Signup and view all the answers

In Class A GPCRs, what structural change occurs when a ligand binds?

<p>TM2 rotates and swings away (C)</p> Signup and view all the answers

What kind of conformations are shown in Figure 6 representing structural rearrangements during GPCR activation?

<p>Inactive and active conformations (B)</p> Signup and view all the answers

What are the distinct regions of the GPCR highlighted in Figure 6 for differences in helix position and side-chain orientation?

<p>The binding pocket and the intracellular coupling site (A)</p> Signup and view all the answers

What characterizes the transmembrane domain of the GPCR?

<p>Membrane helices and three extracellular loops (A)</p> Signup and view all the answers

What does TM6 do when a ligand binds in Class A receptors?

<p>Rotates and swings away from the center (C)</p> Signup and view all the answers

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