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- 1. Ionotropic GABA receptors are ligand-gated Cl channels which open during GABA-ergic signaling. a) Describe how under normal circumstances the opening of these channels leads to an IPSP. Do this in the context of Eci. b) Some cells in the body express a Na*/K+/2Cl cotransporter which pumps Cl- into the ICF. Where these pumps are present, the same GABA receptor is actually excitatory. Again, in the context of Ea describe how the same receptor would be excitatory in cells which actively pump Cl- into the ICF. You do not need to repeat information you provided in part (a)Estimate the binding affi nity of a ligand for its receptor from the followingdata:Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium. They have an important role in vascular homeostasis. Endothelin activates G protein-coupled receptors (GPCRs) ETA or ETB on a target cell. Which subunit of heterotrimeric G protein is released when the receptor is activated? a.) gamme b.) beta c.) alpha
- 3) Acetylcholine binds to a GPCR on heart muscle, making the heart beat more slowly. The activated receptor stimulates a G protein, which opens a K+ channel in the plasma membrane, as shown in Figure 1. Which of the following would enhance this effect of the acetylcholine? (a) (b) (c) (d) Figure 1 addition of a high concentration of a non-hydrolyzable analog of GTP addition of a drug that prevents the a subunit from exchanging GDP for GTP mutations in the acetylcholine receptor that weaken the interaction between the receptor and acetylcholine mutations in the acetylcholine receptor that weaken the interaction between the receptor and the G protein5.. A sample of cells has a total receptor concentration of 25 mM. Ninety percent of the receptors have bound ligand and the concentration of free ligand is 125 µM. Calculate the K for the receptor ligand interaction. (a) What is the AG° for binding for this interaction at 25°C?α-Bungarotoxin is a powerful neurotoxin found in the venom of a poisonous snake (Bungarus multicinctus). It binds with high specificity to the acetylcholine receptor (AChR; an integral membrane protein) andprevents its ion channel from opening. This interaction was used to purify AChR from the electric organ of torpedo fish.(a) Outline a strategy for using α-bungarotoxin covalently bound to chromatography beads to purify the AChR protein. (b) Outline a strategy for the use of [125I]α-bungarotoxin to purify the AChR protein.
- 6. For a 1:1 ligand-receptor binding interaction that is modeled by X + Y XY : (A) Show how the fraction of ligand-receptor binding (fo) is represented by the [X] [X]+ K, equation of f, (i.e., derive this expression for this reaction beginning eg with the relationship for K = f([X].[X],[XY]) under equilibrium conditions). (B) shown to the right for this reaction, what is the estimated value of Keg? Give your answer in units of M. For the data plot 0.9 0.8 0.7 0.6 문 0.5 0.4 0.3 0.2 0.1 0.0000 0.0050 0.0100 0.0150 0.0200 0.0250 0.0300 0.0350 0.0400 [X) (mM)2) After plotting actin bound to cofilin versus the cofilin concentration, you generate the figure below. v (cofilin binding density) 1 0.8 0.6 0.4 0.2 0 2 4 6 8 [S. pombe cofilin] free (UM) 10 a) What is the Kd you measure for this interaction? b) What is the AG of the interaction? c) Based on the data, is there anything you suspect about the binding of protein and ligand?A) Please explain what a G protein coupled receptor is. Please explain how G protein interacts with this receptor. B) Please explain the kind of reactions that follow binding a specific ligand to a G protein coupled receptor. What do these reactions do in the cell? C) How do these reactions work in the cell. What is the function of these reactions in the cell? How do the reactions proceed?
- The top panel (a) of this figure shows the graded potential change (far right, upper, electrical trace) that results from ligand binding to the ligand gated Na+ channel. The bottom panel of this figure (b) shows a graded potential change (far right, lower, electrical trace) that results from ligand binding to a ligand gated Cl- channel. From this trace you know (Vm = -70 mV) 1. ECl- is -70 mV 2. ECl- is more negative than -70 mV (i.e., -80 mV) 3. ECl- is more positive than -70 mV (i.e., -60 mV)19. Which of the following statements is FALSE? A) Nucleotides and amino acids can act as extracellular signal molecules. B) Some signal molecules can bind directly to intracellular proteins that bind DNA and regulate gene transcription. C) Some signal molecules are transmembrane proteins. D) Answer: Dissolved gases such as nitric oxide (NO) can act as signal molecules, but because they cannot interact with proteins they must act by affecting membrane lipids. Explanation:6. Increasing the aldosterone secretion during prolonged muscle activity in hot weather allows you to compensate for the sodium loss in sweat and remove the accumulated excess of potassium. Explain these biological effects of the hormone during exercise. For answer: „Total Signal transduction starting with hormon recopios, e) explain the role of the hormone in the regulation of gene transcription and translation; d) describe the role of proteins that have their synthesis regulated by aldosterone.
