BMC3031 - Chemistry of Drug Action

Leader: Dr. Philip Thompson

Offered

Parkville First semester 2007 (Day)

Synopsis

This unit examines the different mechanisms of action by which drugs exert their biological activity. In particular, the unit will address the interactions between endogenous ligands (eg. neurotransmitters, peptides and proteins, lipids, carbohydrates) with their macromolecular targets such as receptors, enzymes and nucleic acids, and the way that drugs mimic, oppose or modify those interactions.

The unit will be divided into sections relating to targets, drugs that act at receptors, drugs that act upon enzymes, drugs that interact with oligonucleotides.

Objectives

At the completion of this unit the participant will be able to:

1. Identify the common classes of receptor.
2. Define a receptor agonist, antagonist, inverse agonist and allosteric modulator.
3. Cite examples of how compounds acting at receptors act as therapeutic agents.
4. Describe various classes of enzymes by the reactions they catalyze.
5. Show an understanding of the kinetic properties of enzymes.
6. Describe the utility of substrate analogues, transition state analogues, and irreversibly binding compounds as enzyme inhibitors.
7. Cite examples of how enzyme inhibitors act as therapeutic agents.
8. Understand the importance of oligonucleotide structure to protein expression.
9. Show how ligands can recognize and modify DNA tertiary structure.
10. Explain the principles governing the anti-sense approach to drug design.
11. Cite examples of how compounds acting at oligonucleotides act as therapeutics.
12. Distinguish ligand-based design, structure-based design and mechanism-based design strategies.
13. Understand the principles governing the generation of small molecule structure activity relationships
14. Understand approaches to peptidomimetic design

Assessment

End of semester exam: 60% (2.5 hours), Mid-semester exercise (10%), Practical class and reports (30%)

Prerequisites

BMC2021, BMC2022, BMC2032

Co-requisites

The other core compulsory Units of the Bachelor of Medicinal chemistry