Monash University Handbook 2010 Undergraduate - Unit

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.

This will involve the study of:

• G-protein coupled receptors
• Other Receptor types
• Ion Channels
• Nuclear Hormone Receptors
• Drugs interacting with Oligonucleotides
• Enzyme and Enzyme Inhibition
• Metal Ions in Enzymes and in Nucleic Acid Targeted Drugs

Objectives

At the end of this unit students will be able to:

1. identify the common classes of receptor and link this to an ability to define receptor agonists, antagonists, inverse agonists and allosteric modulators. In addition students will be able to cite examples of how compounds acting at receptors act as therapeutic agents.
2. describe various classes of enzymes by the reactions they catalyse and show an understanding of the kinetic properties of enzymes.
3. describe the utility of substrate analogues, transition state analogues, and irreversibly binding compounds as enzyme inhibitors. This will also be linked to an ability to understand how enzyme inhibitors act as therapeutic agents.
4. describe the role of metal ions in enzymatic processes.
5. show how platinum-based drugs interact with oligonucleotides to disrupt cell processes and link this to an understanding of the importance of oligonucleotide structure to protein expression.
6. show how ligands can recognize and modify DNA tertiary structure and link this with an ability to cite examples of how compounds acting at oligonucleotides function as therapeutics.
7. distinguish ligand-based design, structure-based design and mechanism-based design strategies.
8. understand the principles governing the generation of small molecule structure activity relationships.
9. understand approaches to peptidomimetic design.
10. acquire skills in researching information and to present the findings in a structured, logical and fluent manner.
11. be proficient in chemical laboratory techniques and communicating the results in written form.

Assessment

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

Chief examiner(s)

Dr David Manallack

Contact hours

36 1 hour lectures and nine 4 hour practicals

Prerequisites

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

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

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