Module summary active learning

Question 1

Describe and give examples of the four main classes of proteins targeted by drugs in mammalian cells. Identify drug targets from the following list

A) Voltage-gated sodium channels
B) mRNA
C) Mu Opioid receptor
D) Cyclooxygenase
E) cAMP

Answer 1

A) Voltage-gated sodium channels
C) Mu Opioid receptor
D) Cyclooxygenase

Question 2

Define drugs classed as ‘biopharmaceuticals’ and describe how these differ from conventional small molecule drugs. Which of the following statements about Biopharmaceuticals is CORRECT?

A) Generally drugs have a molecular weight >5000 kDa
B) Usually a predictable relationship between dose and effect
C) long half life, atypical biodistribution and removal mechanisms
D) drug interactions may be cause of toxicity
E) adverse effects associated with immunogenicity

Answer 2

A) Generally drugs have a molecular weight >5000 kDa
C) long half life, atypical biodistribution and removal mechanisms
E) adverse effects associated with immunogenicity

Question 3

Describe canonical signalling mechanisms used by receptors commonly targeted by drugs to bring about changes in cell function. Which of the following signalling mechanisms are CORRECT?

A) cation influx across the plasma membrane, depolarisation and action potential firing
B) GTP exchange for GDP on Gs alpha subunit, dissociation of alpha and beta gamma subunit, GTP-bound Gs subunit binding to adenylate cyclase, increased synthesis of cAMP, activation of PKA, phosphorylation of target proteins
C) GTP exchange for GDP on Gi alpha subunit, dissociation of alpha and beta gamma subunit, GTP-bound Gi subunit binding to phosphodiesterase, increased breakdown of cAMP, dephosphorylation of target proteins
D) GTP exchange for GDP on Gq alpha subunit, dissociation of alpha and beta gamma subunit, GTP-bound Gq subunit binding to phospholipase C, PIP2 breakdown and generation of IP3 and DAG, increased intracellular calcium, activation of calcium regulated proteins
E) increased intracellular calcium, activation of calcineurin, dephosphorylation of NFkappaB, translocation to the nucleus

Answer 3

A) cation influx across the plasma membrane, depolarisation and action potential firing
B) GTP exchange for GDP on Gs alpha subunit, dissociation of alpha and beta gamma subunit, GTP-bound Gs subunit binding to adenylate cyclase, increased synthesis of cAMP, activation of PKA, phosphorylation of target proteins
D) GTP exchange for GDP on Gq alpha subunit, dissociation of alpha and beta gamma subunit, GTP-bound Gq subunit binding to phospholipase C, PIP2 breakdown and generation of IP3 and DAG, increased intracellular calcium, activation of calcium regulated proteins
E) increased intracellular calcium, activation of calcineurin, dephosphorylation of NFkappaB, translocation to the nucleus

Question 4

What is the definition of these terms?
1) the ability of a drug to bind to a receptor
2) The proportion of receptors to which a drug is bound
3) Relative affinity or activity of a drug between different receptor types
4) The ability of an agonist to elicit a response following binding
5) A measure of the concentration of a drug (agonist or antagonist) at which it is effective

Answer 4

1) Affinity
2) Occupancy
3)Selectivity
4)Efficacy
5)Potency