VPS3091 - Molecular basis of drug action

Leader(s): Dr David Manallack

Offered

Parkville First semester 2009 (Day)

Synopsis

This unit will introduce students to the different mechanisms of action by which drugs exert their biological activity. It will address the interactions between endogenous ligands and drugs with their receptors, enzymes or nucleic acids, and the way that drugs mimic, oppose or modify those interactions. Students will be introduced to the scope of medicinal chemistry techniques used in contemporary drug discovery.

Objectives

On completion of this unit student 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 catalyse;
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. Describe the role of metal ions in enzymatic processes;
9. Show how platinum-based drugs interact with oligonucleotides to disrupt cell processes;
10. Understand the importance of oligonucleotide structure to protein expression;
11. Show how ligands can recognize and modify DNA tertiary structure;
12. Cite examples of how compounds acting at oligonucleotides act as therapeutics;
13. Distinguish ligand-based design, structure-based design and mechanism-based design strategies;
14. Understand the principles governing the generation of small molecule structure activity relationships;
15. Understand approaches to peptidomimetic design.

Assessment

poster presentation: 10%; practical sessions and reports: 20%; final exam: 70%

Contact hours

36 1 hour lectures and nine 4 hour practicals

Prerequisites

PSC1021 (or VPS1021) Organic chemistry I
PSC1022 (or VPS1022) Organic chemistry II
VPS2062 Pharmacology
VPS2011 Pharmaceutical biochemistry
VPS2092 Molecular cell biology

Additional information on this unit is available from the faculty at:

http://www.monash.edu.au/muso/