Which of the following is the best description of how a G protein coupled receptor responds to a ligand binding? Binding of ligand to the receptor causes the G protein to swap out GTP for GDP Binding of ligand to the receptor causes the G proteins to dimerize and trigger cross-phosphorylation Binding of ligand to the receptor causes the G protein to become activated, then the G protein travels through the plasma membrane to activate an enzyme Binding of ligand to the G protein triggers it to swap out GDP for GTP, causing it to become activated
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- You learned in this chapter that Na+/K+ active transport pumps in the plasma membrane of the axons are responsible for creating the imbalance between Na+ and K+ inside and outside of the neuron that produces the resting membrane potential. In early research studying the role of ions and the involvement of active transport of ions in neural signaling, investigators used the giant axon of a squid as a model. The diameter of a giant axon is far greater than that of a mammalian axon, which enabled researchers to isolate it easily and use it in in vitro experiments. In one early experiment, researchers investigated the active transport of Na+ out of the axon in response to the presence of cyanide. Experimentally they hooked up a section of axon to a syringe, immersed the axon in artificial seawater, introduced radioactive 22Na (as 22NaCl) into the axon, and then quantified the transport of 22Na out through the axons plasma membrane. The rate of 22Na transport out of the axon was determined by measuring the radioactivity released into the fluid sur- rounding the axon over a period of time. The Figure shows the results of the experiment. What is the effect of cyanide on Na1 transport out of the squid axon? How do the data show the effect? Source: P. C. Caldwell et al. 1960. The effects of injecting energy-rich phosphate compounds on the active transport of ions in the giant axons of Loligo. The Journal of Physiology 152:561590. Cengage Learning 2017Figure 9.8 HER2 is a receptor tyrosine kinase. In 30 percent of human breast cancers, HER2 is permanently activated, resulting in unregulated cell division. Lapatinib, a drug used to treat breast cancer, inhibits HER2 receptor tyrosine kinase autophosphorylation (the process by which the receptor adds phosphates onto itself), thus reducing tumor growth by 50 percent. Besides autophosphorylation, which of the following steps would be inhibited by Lapatinib? Signaling molecule binding, dimerization, and the downstream cellular response. Dimerization, and the downstream cellular response. The downstream cellular response. Phosphatase activity, dimerization, and the downsteam cellular response.Which of the following statements most accurately describes what happens when an antagonist binds to a receptor? The antagonist binds non-covalently to the receptor and promotes internalisation of the receptor. Antagonist binding alters the structure of the receptor making it unable to function normally. At sufficiently high concentrations the antagonist can prevent the receptor from binding to its natural (endogenous) ligand. The antagonist-receptor complex binds to a heterotrimeric G protein forming a stable and inactive ternary complex.
- A drug binds to a receptor and causes an immediate change in the electrical signaling or excitability of that cell, without activating another signaling molecule. What type of receptor is this drug most likely binding to? G-protein coupled receptor (GPCR) Ligand-gated ion channel Enzyme-coupled receptor Intracellular receptor Voltage-gated ion channelWhich of the following is true of signal transduction mediated by protein tyrosine kinases production of cAMP phosphoinositides are activated arrestins compete with G-proteins phosphorylation of tyrosine residuesWhich of the following would inhibit the activity of TGF-Beta receptor? multiple answers A. Deletion of Extracellular domain B. Tyrosine Kinase Inhibitor C. Mutation that prevents homodimerization of Type II Receptor D. Mutation of phosphorylation site on Type I receptor E. Inhibition Type II receptor binding to Type I receptor
- For a signal to be sent down an axon of a nerve cell, an action potential must be generated. This is done by.. Select one: a. G-protein coupled receptors bind ligand, a phosphorylation cascade occurs, this causes a change in charge of the membrane due to the addition of phosphates allowing Na+ channels to open. b. Ligand-gated K+ channels open, allowing K+ to rush out of the cell and depolarize that part of the membrane. This change in charge opens neighboring voltage-gated channels. c. Ligand-gated Na+ channels open, allowing Na+ to rush in. This then depolarizes that region of the membrane resulting in opening neighboring voltage-gated channels. d. Receptor tyrosine kinases have two Na+ molecules bind, this opens voltage-gated channels allowing the “signal” to pass down the axon.Which of the following statements best defines the term ‘spare receptors’? ‘Spare receptors’ refers to receptors that are broken down by cells because they are surplus to requirements. ‘Spare receptors’ occur when the KD for agonist binding to the receptor is smaller than the EC50 determined for a particular physiological response. ‘Spare receptors’ refers to the pool of intracellular receptors that are able to translocate to the plasma membrane. ‘Spare receptors’ can be defined as the number of receptors not occupied by agonist when a maximal response has been achieved, compared to the total number of receptors in the cell.All cells of a multicellular organism may not respond in the same wayto a particular ligand (signaling molecule) that binds to a cell surfacereceptor. The difference in response may be due toa. the type of receptor for the ligand that the cell expresses.b the affinity of the ligand for the receptor in a given cell type.c. the type of signal transduction pathways that the cell expresses.d. the type of target proteins that the cell expresses.e. all of the above.
- Cholera toxins, produced by the pathogenic bacteria Vibrio cholerae, disrupt G Protein Coupled Receptor (GPCR) signaling pathways. They interfere with... the ability of the beta subunit of a G protein to bind to the GPCR the ability of the gamma subunit of a G protein to exchange GDP for GTP the ability of the beta subunit of a G protein to bind to an effector protein the ability of the alpha subunit of a G protein to hydrolyze GTP to GDPName three features common to the activation of cytokine receptors and receptor tyrosine kinases. Name one difference with respect to the enzyme activity of these receptors.The G protein coupled receptor (GPCR) pathway elicits diverse intracellular responses in different cells. The basic steps of GPCR signaling are outlined in this diagram. Which of the following statements correctly describes the process of GPCR signaling? The GPCR activation is reversible after the signal of the ligand diminishes. The membrane-embedded enzyme uses GTP as a secondary messenger to initiate gene expression. The ligand attaches to both the GPCR and the membrane-embedded enzyme to activate the GPCR pathway. The ligand-bound GPCR sends a GTP molecule to an enzyme in the membrane and switches it into an active state.