2024/25 Taught Postgraduate Module Catalogue

CHEM5107M Modern Drug Discovery

15 creditsClass Size: 65

Module manager: Dr Richard Foster
Email: r.foster@leeds.ac.uk

Taught: Semester 1 (Sep to Jan) View Timetable

Year running 2024/25

Pre-requisite qualifications

None

Module replaces

None

This module is not approved as an Elective

Module summary

The entire process of drug discovery will be covered, providing a broad context before concentrating upon the details of small molecule drug discovery (however, structure-based drug discovery will be covered in detail in a separate module). The module starts with looking at the major scientific milestones that have enabled modern disease-based and target-based drug discovery. Starting with the identification and validation of potential new drug targets, appropriate biochemical and pharmacological assays are employed alongside large libraries of small molecule compounds to identify initial “hits”. Iterative rounds of medicinal synthetic chemistry and analytical pharmacological analysis, are used to explore and enhance compound potency or efficacy in order to generate lead compounds. Medicinal chemistry is used further to optimise the lead compound to reduce potential toxicity and to enhance the pharmacokinetic profile, while maintaining efficacy/potency. A successful programme will eventually lead to a candidate drug that can enter preclinical drug development. The module will study the chemical and pharmacological principles and methodologies underlying all these processes.

Objectives

The module will teach key techniques and strategies used in designing effective small molecule-based therapeutics. The module will describe new methods to identify ‘hits’ and improve ‘drug-like’ properties to generate ‘leads’ and ‘optimised leads’ leading to the generation of clinical candidates. Key units will teach the importance of pharmacokinetics and how best to mitigate for toxicity during the optimisation process. The course will also introduce the important concept of intellectual property and patent protection in the pharmaceutical industry.

Learning outcomes
On completion of this module, students should be able to demonstrate the following learning outcomes as evidenced by the ability to answer deductive questions related to the module material and to communicate in the form of a scientific poster, how the relevant principles of drug discovery apply to an example industrial case study:
1. Understand the modern drug discovery process and how it has developed;
2. Define the stages of target-based small molecule drug discovery, including: target identification, target validation, HTS and hit identification, lead discovery, lead optimisation;
3. Understand the principle modes of binding of small drug molecules to biological macromolecules and identify key recognition features in drug molecules;
4. Understand the role of the Structure Activity Relationship and the importance of the pharmacophore and how QSAR is used to increase the efficiency of the drug design process;
5. Understand how lead optimisation is used to avoid drug toxicity;
6. Explain how in vitro and in vivo pharmacokinetic assessments are used to assess DMPK;
7. Have knowledge of Intellectual Property and how to define what is patentable with respect to chemical structures;
8. Use examples and case studies of drug discovery to explain how principles of modern drug discovery is used in the pharmaceutical industry.

Syllabus

Drug discovery pathways; Milestones enabling modern drug discovery; The context of classical small molecule drug discovery in the broader context of the pharmaceutical industry; Compound sources and libraries; Pharmacological and biochemical assays used to measure target interaction and selectivity; High throughput screening to identify credible small molecule “hit” compounds; Lead Generation – medicinal chemical approaches to enhance target interaction and selectivity; Quantification of structure activity relationships and pharmacophores; Lead Optimisation - avoiding drug toxicity; DMPK: in vitro and in vivo pharmacokinetic assessments; Intellectual property – what is patentable?; Case studies of drug discovery.

Teaching methods

Delivery type	Number	Length hours	Student hours
Workshop	3	2.00	6.00
Workshop	5	1.00	5.00
Office Hour Discussions	5	1.00	5.00
presentation	1	2.00	2.00
Seminar	1	1.00	1.00
Independent online learning hours			16.00
Private study hours			115.00
Total Contact hours			19.00
Total hours (100hr per 10 credits)			150.00

Private study

125h including 25h online study - quizzes, note-taking, additional reading and research

Opportunities for Formative Feedback

Example problems in workshops and online quizzes associated with learning units will provide formative feedback.

Methods of assessment

Coursework

Assessment type	Notes	% of formal assessment
Poster Presentation	Group poster presentation	33.00
In-course MCQ	In-course MCQ	33.00
Problem Sheet	Deductive problem sheet	34.00
Total percentage (Assessment Coursework)		100.00

Interdisciplinary teamwork to make a poster presentation illustrating the development of a drug.

Reading list

There is no reading list for this module

Last updated: 18/07/2024

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