Pharmacology 4D03: Drug Design
COORDINATOR EVA WERSTIUK Ext. 22204
Office: HSC 4N39
Drug Design Course Overview
The problems developed for this course offer students the opportunity for self-directed learning in a broad area of pharmacology with special emphasis on the molecular mechanisms and structure-activity relationships of the drugs studied. Apart from "personal" objectives, there are minimal course objectives (described below) that each student will be expected to attain.
Minimal Course Objectives
Part A
i) Discuss the molecular mechanism of action of five of the following types of drugs:
- Beta-Lactam antibiotics
- DNA synthesis inhibitors
- HIV protease inhibitors
- Adenosine receptor agonists/antagonists
- Excitatory amino acid receptor agonists/antagonists
- Angiotensin converting enzyme inhibitors
- Receptor-tyrosine kinase inhibitors
ii) Demonstrate an understanding of the concepts involved in designing drugs for selected target sites, such as: cell-membrane receptors; intracellular or extracellular enzymes; receptor-coupled signal transduction pathways; bacterial cell wall synthesizing enzymes, viral proteases and viral nucleic acids synthesising enzymes.
Part B
i) Demonstrate an understanding of the physicochemical principles involved in drug action by being able to discuss how the following parameters influence drug action:
- Stereochemistry and conformation
- Electronic structure
- Nature of chemical bonding
ii) Apply these concepts to novel systems in a final written examination.
Part C
i) Demonstrate an understanding of the concepts and principles of drug design by being able to discuss current approaches employed in the design of new drugs:
- Discovery of lead compounds - natural products as pathfinders
- High-throughput screening - a tool for drug discovery
- Identification of drug targets - application of molecular biology and bioinformatics
- Structure modification - the generation of combinatorial libraries
- Structure based drug design - the process of iterative optimisation
ii) Apply these concepts to novel systems in a final written examination.
A) i) Discuss the molecular mechanism of action of five of the following types of drugs:
<!--[if !supportLists]-->2. <!--[endif]-->b-Lactam antibiotics
<!--[if !supportLists]-->3. <!--[endif]-->DNA synthesis inhibitors
<!--[if !supportLists]-->4. <!--[endif]-->HIV protease inhibitors
<!--[if !supportLists]-->5. <!--[endif]-->Adenosine receptor agonists/antagonists
<!--[if !supportLists]-->6. <!--[endif]-->Excitatory amino acid receptor agonists/antagonists
<!--[if !supportLists]-->7. <!--[endif]-->Angiotensin converting enzyme inhibitors
<!--[if !supportLists]-->8. <!--[endif]-->Receptor-tyrosine kinase inhibitors
ii) Demonstrate an understanding of the concepts involved in designing drugs for selected target sites, such as: cell-membrane receptors; intracellular or extracellular enzymes; receptor-coupled signal transduction pathways; bacterial cell wall synthesizing enzymes, viral proteases and viral nucleic acids synthesising enzymes.
