PSC3111 - Molecular basis of drug action - 2017

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
• enzymes and enzyme inhibition

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 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;
6. Distinguish ligand-based design, structure-based design and mechanism-based design strategies;
7. Understand the principles governing the generation of small molecule structure activity relationships;
8. Understand approaches to peptidomimetic design;
9. acquire skills in researching information and to present the findings in a structured, logical and fluent manner;
10. Be proficient in chemical laboratory techniques and communicating the results in written form.

Final exam 60%; poster presentation: 15%; practical sessions, reports and other assessments 25%

Contact hours for on-campus students:

• Thirty two 1-hour lectures
• Four 3-hour practicals/workshops

See also Unit timetable information

Dr David Manallack

PSC2011 Pharmaceutical biochemistry

PSC2021 Structural Organic Chemistry

http://www.monash.edu/pharm/current/