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Patrick: an Introduction to Medicinal Chemistry 5E Chapter 04 Patrick: An Introduction to Medicinal Chemistry 5e Chapter 04 01) Which of the following statements is not true about receptors? a. Most receptors are proteins situated inside the cell. b. Receptors contain a hollow or cleft on their surface which is known as a binding site. c. Receptors bind chemical messengers such as neurotransmitters or hormones. d. Receptors do not catalyse reactions on chemical messengers. 02) Which of the following statements is not true? a. Neurotransmitters are released by nerves. b. Neurotransmitters are required to carry a 'message' from a nerve to a target cell. c. Neurotransmitters only have small distances to cover to reach their target cells. d. Neurotransmitters bind to receptors within target cells. 03) Which of the following is not a neurotransmitter? a. Glycine. b. Cyclic GMP. c. -Aminobutyric acid. d. Serotonin. 04) Which of the following statements is not true regarding the binding site of a receptor? a. The binding site is normally a hollow or cleft in the surface of a receptor. b. The binding site is normally hydrophilic in nature. c. Chemical messengers fit into binding sites and bind to functional groups within the binding site. d. The binding site contains amino acids which are important to the binding process. 05) Which of the following amino acid residues is likely to form its strongest binding interaction by means of: (valine, glycine, serine, aspartate) a. Hydrogen bonding b. Ionic bonding c. Van der Waals interactions d. None of these options (only one) 06) Which of the following statements best describes an induced fit? a. The process by which a binding site alters shape such that it is ready to accept a chemical messenger. b. The process by which a chemical messenger adopts the correct binding conformation before entering a binding site. c. The process by which binding of a chemical messenger to a binding site alters the shape of the binding site. d. The process by which a binding site alters the shape of the chemical messenger into the binding conformation before binding. 07) Which of the following amino acid residues is likely to form its strongest binding interaction by means of: (alanine, threonine, glysine, lysine) a. Hydrogen bonding b. Ionic bonding c. Van der Waals interactions d. None of the answers © Oxford University Press, 2013. All rights reserved. Patrick: An Introduction to Medicinal Chemistry 5e Chapter 04 08) There is a fine balance required for the binding interactions of a neurotransmitter with its receptor. Which of the following statements best expands on this statement? a. It is important that the binding interactions involve a mixture of van der Waals interactions, hydrogen bonds and ionic bonds since neurotransmitters have different functional groups. b. The binding interactions must be of the correct nature to match the functional groups of the neurotransmitter and the functional groups in the binding site. c. The binding interactions must be sufficiently strong that the neurotransmitter binds long enough to have an effect, but not too strong in case the neurotransmitter remains permanently bound. d. There must be the correct balance of hydrophilic and hydrophobic interactions to ensure that the chemical messenger can enter a hydrophobic binding site. 09) When a membrane-bound receptor binds its chemical messenger, an induced fit takes place which leads to secondary effects, allowing a chemical message to be received within the cell. Which of the following mechanisms is not involved in this process? a. The transport of the chemical messenger into the cell. b. The opening or closing of an ion channel. c. The activation of a signal protein. d. The activation of a membrane-bound enzyme. 10) Which of the following statements is not true about a ligand-gated ion channel receptor? a. Ligand-gated ion channel receptors are present in the cell membrane. b. Neurotransmitters can act as the chemical messengers for ligand-gated ion channels. c. Ligand-gated ion channels consist of six glycoproteins. d. Some ion channel receptors are controlled by differences in membrane potential rather than by ligands. 11) Which of the following statements is not true about ligand-gated ion channels? a. There are different ligand-gated ion channels for specific ions. b. The response time to a neurotransmitter is slow. c. The process by which an ion channel opens as a result of receptor-ligand binding is known as gating. d. The opening of cationic ion channels generally leads to depolarisation of the cell. 12) Which of the following statements is true about the ion channel controlled by the nicotinic receptor? a. Each protein subunit of the ion channel contains three hydrophobic regions which traverse the cell membrane. b. Three of the protein subunits are identical (the -subunits). c. The binding site for the nicotinic receptor is located solely on the -subunit which means that there are two binding sites per ion channel. d. Each protein subunit of the ion channel has a lengthy N-terminal extracellular chain. 13) The nicotinic receptor controls an ion channel. Which of the following statements is true about the -subunit of this ion channel? a. The N-terminal and C-terminal chains are both intracellular. b. There is one intracellular loop. c. The binding site for the neurotransmitter resides solely on the N-terminal chain. d. There are two extracellular loops © Oxford University Press, 2013. All rights reserved. Patrick: An Introduction to Medicinal Chemistry 5e Chapter 04 14) The mechanism of gating involves the rotation of five kinked -helices which traverse the cell membrane. Which of the following statements is untrue? a. Each protein subunit making up the ion channel contributes one of the kinked -helices. b. It is the -helix of the first transmembrane section that is involved. c. Rotation of the helices opens up a central channel to allow the flow of ions. d. The neurotransmitter binds to the N-terminal chain to produce a rapid response. 15) Which of the following statements is true about a G-protein coupled receptor? a. It contains five transmembrane hydrophobic sections. b. There are more extracellular loops than intracellular loops. c. The binding region for the G-protein involves one of the intracellular loops and the C- terminal chain. d. The N-terminal chain is intracellular and the C-terminal chain is extracellular. 16) Which of the following is not a G-protein coupled receptor? a. The histamine receptor. b. The nicotinic receptor. c. The dopaminergic receptor. d. The adrenergic receptor. 17) Which of the following statements is not true about G-protein coupled receptors? a. They contain seven transmembrane sections. b. They mediate the action of some hormones. c. They activate signal proteins called G-proteins. d. Growth factors can act as ligands for some G-protein coupled receptors. 18) Which of the following pairs of receptors illustrates convergent evolution? a. The D1B and D1A dopaminergic receptor subtypes. b. The H1 and H2 receptor subtypes. c. The 2a and 2b adrenoceptor subtypes. d. The M2 and M4 muscarinic receptor subtypes. 19) Which of the following statements is true about a tyrosine kinase linked receptor? a. It is situated in the cytoplasm. b. The N-terminal chain is intracellular. c. The ligand binding site is in the C-terminal chain. d. It has one hydrophobic transmembrane region. 20) Which of the following is a messenger for a tyrosine kinase linked receptor? a. Adrenaline. b. Dopamine. c. Epidermal growth factor. d. Histidine. 21) Which of the following statements is untrue regarding the epidermal growth factor receptor? a. Binding of epidermal growth factor results in dimerisation of the receptor. b. Dimerisation activates the kinase active site. c. Activation of the kinase results in phosphorylation of serine residues. d. One half of the receptor dimer catalyses reactions on residues present on the other half. © Oxford University Press, 2013. All rights reserved. Patrick: An Introduction to Medicinal Chemistry 5e Chapter 04 22) Which of the following statements is true regarding intracellular receptors? a. They consist of three protein subunits. b. They contain a ligand binding site near the N-terminal end. c. They contain a binding region for DNA near the middle of the protein. d. They are activated by hydrophobic molecules which are synthesised within the cell. 23) Which of the following statements is true regarding the DNA binding region of intracellular receptors? a. It contains nine cysteine residues. b. Four cysteine residues are involved in binding two zinc ions. c. It contains particular nucleotide sequences that can base pair to DNA. d. The DNA binding region is known as having 'thiol fingers'. 24) Which of the following statements is not true about a ligand-gated ion channel receptor? a. Ligand-gated ion channel receptors are present in the cell membrane. b. Neurotransmitters can act as the chemical messengers for ligand-gated ion channels. c. Ligand-gated ion channels consist of five glycoproteins. d. Differences in membrane potential affect whether ligand-gated ion channel receptors open or close. 25) Which of the following statements is not true about ligand-gated ion channels? a. There are different ligand-gated ion channels for specific ions. b. The response time to a neurotransmitter is extremely fast. c. The process by which an ion channel opens as a result of receptor-ligand binding is known as gating. d. The opening of cationic ion channels generally leads to polarisation of the cell. 26) Which of the following statements is true about the ion channel controlled by the nicotinic receptor? a. Each protein subunit of the ion channel contains three hydrophobic regions which traverse the cell membrane. b. Two of the protein subunits are identical (the -subunit). c. The binding site for the nicotinic receptor is located solely on the -subunit which means that there are two binding sites per ion channel.
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