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 strategy 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) designing 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 medicine 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. Finally 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.

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: 3
discuss approaches to rational drug design based on knowledge of the three-dimensional structure of biological targets: 3
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

Study hours

8 hours in-situ workshops/tutorials supporting lecture content
12 hours IT workshops
02 hours examination
80 hours private study to support asynchronous activity including preparations for workshops, directed reading and additional resources, exam preparartion
48 hours private study: preparation of in-course assessments

School Rules

None

Description of Module Assessment

1: Report weighted 20%
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

2: Group Project weighted 20%
Group communication exercise
Working in groups (2-3) students will produce a product information leaflet on an allocated pharmaceutical detailing key information on the structure, function and biological activity of the molecule

3: Open Book Examination weighted 60%
Online open book exam
The paper will be released on KLE as a Word document at 9am on the morning of the exam. Examination consisting of two sections; A) a short answer/MCQ section (50% of the examination) B) essay question (50% of the examination). Students should answer each question using Word, clearly labelling each question as they provide their answers. Work will be submitted to Turnitin no later than 5pm on the day of release. International students will be asked to notify the School if they need an extension due to different time zones. Although students have been given significant time to complete this exam script, we expect most students to spend no more than 2 hours. Answers should be as accurate and concise as possible. For short-answer questions, students should pay careful attention to the number of points that each question is worth. In general, we would expect only one or two sentences for each point. For essay-based questions, typical answers would be in the range of 500-750 words per question. We recommend that students do not exceed 750 words per essay-based question as we will be assessing the quality of your answer, not the quantity.