LSC-20087 - Drug design
Coordinator: Anja Winter Tel: +44 1782 7 33117
Lecture Time: See Timetable...
Level: Level 5
Credits: 15
Study Hours: 150
School Office: 01782 734414

Programme/Approved Electives for 2022/23

None

Available as a Free Standing Elective

No

Co-requisites

None

Prerequisites

none

Barred Combinations

none

Description for 2022/23

Many drugs that are available today were discovered by chance through the 'trial-and-error' method. Current drug discovery, however, utilises the vast amount of information that is available through genomics, proteomics and structural studies. One of the most common strategies in drug discovery is the use of structure-based drug design. The rational development of a new drug therefore follows the following steps:
i) identification of a biological target, such as a receptor or an enzyme that is related to a particular disease
ii) design of a molecule that binds to the target and has the desired biological effect on the target.
This process can take several years to bring a pharmaceutical from the bench to the patient. Even with very good information of the structure of the target, it is very difficult to design a drug that will specifically only bind to the selected target and have the desired pharmacological effects. Additionally, pharmacokinetics and drug metabolism are also very important and need to be evaluated.
This module will provide you with an overview of the drug design pipeline starting from in-silico studies up to clinical trials. You will also cover the principles of pharmacokinetics and pharmacodynamics. Specific examples of biological targets will be discussed and you will investigate with the use of informatics tools how chemical structures and biological targets interact. The module assessment will help you to develop and evidence your teamwork and written communication skills to non-specialist audiences in the production of a group patient information leaflet for an allocated pharmaceutical, whilst an individual report will assess your skills in the acquisition and manipulation of structural information for ligand-target interactions, with supporting workshops

Aims
To expand core level 4 biological chemistry material and its application to drug design and development. Students will be introduced to the drug development pipeline through to clinical trials and emerging technologies in drug design, as well as principles of pharmacodynamics and pharmacokinetics, and the physiochemical properties of drugs/ligands and their molecular interactions with biological targets.

Talis Aspire Reading List
Any reading lists will be provided by the start of the course.
http://lists.lib.keele.ac.uk/modules/lsc-20087/lists

Intended Learning Outcomes

explain the principles of the drug discovery pipeline from candidate selection through to clinical trials: 3
explain basic concepts of pharmacokinetics and pharmacodynamics and their importance to drug delivery, potency and selectivity: 2,3
describe the molecular interactions between drugs/ligands and their targets in biological systems: 1,2,3
evaluate the structures of molecules related to their suitability as therapeutic agents and discuss approaches to ligand-based drug design through structure-activity relationships: 1
discuss approaches to rational drug design based on knowledge of the three-dimensional structure of biological targets: 1
manipulate and present structural information for protein-ligand interactions using the protein data bank: 1
communicate effectively in written and visual form through the production of a written report and group communication exercise: 1,2,3

Study hours

8 hours in-situ workshops/tutorials supporting lecture content
12 hours IT workshops
02 hours class test
9x 4 hours engagement with asynchronous activities including preparations for workshops,
46 hours directed reading/engagement with additional resources and private study for class test preparation
46 hours private study: preparation of in-course assessments

School Rules

None

Description of Module Assessment

1: Report weighted 30%
1,000 word report
Students will produce a 1,000 word report assessing the presentation and interpretation of structural data for protein-ligand interactions using the protein data bank/other software for visualisation/manipulation.

2: Group Project weighted 20%
Group communication exercise
Working in groups (2-3) students will produce a patient information leaflet on an allocated pharmaceutical detailing key information on the function and biological activity of the molecule in context to disease treatment.

3: Online Tasks weighted 50%
Class test (1 hour active working in a 2 hour assessment window)
Online class test (1 hour active working in a 2-hour assessment window in the semester 2 exam period), including a mix of MCQ and SAQ-style questions assessing core knowledge of the learning material and the application to drug discovery.