School of Physical and Geographical Sciences  
 
 
CHE-20005 Drug Design Based on biological Targets  
Co-ordinator: Dr Michael Edwards   Tel:33252  
Teaching Team: Dr Graeme  Jones, Mrs Monica  Heaney, Dr Katherine  Haxton, Dr Theresa  Phillips, Miss Nicola  Jervis, Dr Matthew  O'Brien,  Joseph  Harrity,  Nigel  Young  
Lecture Time: See Timetable...  
Level: 2 Credits: 15 Study Hours: 150  
School Office:
 
 
 
Programme/Approved Electives for

None

Available as a Free Standing Elective

No

Prerequisites

Successful completion of Level 1 modules in Chemistry or equivalent

Barred Combinations

None

Description

This is a core module for the medicinal chemistry degree programme at Keele and it develops and exemplifies the principles and methods that relate chemical structure to in vivo transport and biological activity of molecules. Topics covered include structure and function of the cell, basic biochemical processes, cellular building blocks, metabolism and biosynthesis, pharmacodynamics and pharmacokinetics, drug transport illustrated by prodrugs, substituent effects and structure-activity relationships, non-covalent forces and their role in enzyme and receptor binding, receptor classification and dose-response curves. Using these principles, drug design and mechanism of action are illustrated by modern examples of rational drug discovery. The course is taught through lectures, laboratory practicals and problem classes.

Aims

To develop an understanding of the fundamental principles used in medicinal chemistry to provide a deeper insight into the mode of action of medicines.
To develop skills in processing and analysing quantitative chemical and biological data.
To develop experimental and analytical laboratory skills
To develop problem solving and scientific writing skills.


Intended Learning Outcomes

Describe the basic building blocks of biochemistry: aminoacids, peptides, proteins, carbohydrates, fats and lipids; and describe their involvement in drug binding and drug action, and their role in cellular metabolism and biosynthesis.

will be achieved by assessments: 1, 2
Describe and explain enzyme structure and biochemical action and the mechanisms of action of drugs that target enzymes. will be achieved by assessments: 1, 2
Describe the mechanisms and characteristics of the pharmacokinetic concepts of absorption, distribution, metabolism and excretion in relation to drugs. will be achieved by assessments: 1, 2
Apply the principles of pharmacology relating to agonism and antagonism of receptor sites and relate this to structure-activity relationships. will be achieved by assessments: 1, 2
Describe the different receptor types and sub-types, and explain how receptors can initiate a biological response and relate this to drug design concepts. will be achieved by assessments: 1, 2
Describe and analyse the role of structure-activity relationships in drug design with references to specific examples. will be achieved by assessments: 1, 2
Discuss a case history of the discovery and development of at least one drug. will be achieved by assessments: 1, 2
Apply concepts in organic synthesis to access target molecules of interest will be achieved by assessments: 1, 2, 3
Communicate the design, implementation, results and interpretation of practical investigations. will be achieved by assessments: 3

Study hours

Lectures: 20 hours
Class tests: 2 hours
Laboratory practicals and problem classes: 36 hours
Independent study, proforma and lab. notebook preparation: 92 hours



Description of Module Assessment

01: Class Test weighted 20%
In-class test
Students answer questions selected from a bank of seen questions posted on the KLE

02: Unseen Exam weighted 50% (min pass mark of 35)
2 hour unseen examination
The paper is split into two sections with a degree of choice in each section: Part A short answer questions, Part B long answer questions.

03: Laboratory Assessment weighted 30% (min pass mark of 40)
Four pro-forma reports and laboratory notebook
Assessment of the quality of record keeping of experimental results in the students laboratory diary, plus submission of the results of four experiments on proforma's.


Version: (1.06B) Updated: 03/Mar/2013

This document is the definitive current source of information about this module and supersedes any other information.