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:

  1.   Beta-Lactam antibiotics
  2. DNA synthesis inhibitors
  3. HIV protease inhibitors
  4. Adenosine receptor agonists/antagonists
  5. Excitatory amino acid receptor agonists/antagonists
  6. Angiotensin converting enzyme inhibitors
  7. 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:

  1. Stereochemistry and conformation
  2. Electronic structure
  3. 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:

  1. Discovery of lead compounds - natural products as pathfinders
  2. High-throughput screening - a tool for drug discovery
  3. Identification of drug targets - application of molecular biology and bioinformatics
  4. Structure modification - the generation of combinatorial libraries
  5. 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.

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