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Rational Drug Design

Module description

This module explores the biological basis of rational drug design, the deliberate targeting of a particular biological pathway for the treatment of disease. This approach is based on knowledge of the pathophysiology of the disease in question and identification of a suitable molecular target. Targeted drug design also has implications for the personalisation of medicine, through selection of appropriate drugs/therapies for a particular patient based on the molecular signature of their disease, e.g. the use of Herceptin in HER2-overexpressing cancer. You will follow the journey of drug discovery from identification of a potential new drug target (through study of genetics, epigenetics or cell biology), to design of screening assays and high-throughput screening, to approaches taken to test and modify both pharmacokinetic values and biological activity, including chemical group substitution, structure-based drug design, and drug formulation and route of administration. Aspects of drug development (safety, pharmaceutical and clinical development) will also be discussed.
In order to take this module, you must have taken at least one of the following Stage 2 modules: CSC2005 (Introduction to Pharmacology),BIO2088 (Advanced Cell Biology), BIO2090 (Analytical Techniques in Biochemistry), or BIO2092 (Genomics and Introductory Bioinformatics)
This is a core module for students studying BSc(Hons) Medical Sciences (Pharmacology and Therapeutics). It is an optional module for all other BSc Medical Sciences, Biosciences and Flexible Honours students, provided the prerequisites have been met.
Because of the continuously changing pandemic situation, we will plan for online delivery as well. The primary intention is to have as much as possible of the module delivered on campus; if this is not possible, we will move online, with a combination of synchronous and asynchronous activities: lectures will be delivered live on Teams or Zoom apps and students may login live; however, they will be also recorded and can be reviewed by students at any time; there may be additional movies/slides placed online to be consulted at any time by students. If tutorialscannot be delivered on campus, they will be delivered on Teams/Zoom. If the labs cannot be held on campus, we will have recordings with specific experiments to review online.

Module aims - intentions of the module

Taking an interdisciplinary ‘molecules to man’ approach, this module will explore the fundamental principles of the design and development of new pharmacological treatments for human disease, and allow you to practise developing a basic research proposal based on current scientific literature. Module content will examine the spectrum of drug discovery methods, ranging from pure chance to specifically targeted interventions, in particular biological pathways. This module also considers how our rapidly-expanding biomedical knowledge permits a progressive shift towards intended, rather than serendipitous, drug discovery. It further explores how chemical structures can be modified to achieve higher biological efficacy or reduce side effects. The content of this module is intended to build on learning in other modules, such as Introduction to Pharmacology, Disease Diagnostics & Therapeutics, Advanced Cell Biology, Genomics and Introductory Bioinformatics, Analytical Techniques in Biochemistry and Principles of Medical Research. It will also complement other final year modules such as Managing Clinical Trials, and Pharmacology and Medicinal Chemistry.

Intended Learning Outcomes (ILOs)

ILO: Module-specific skills

On successfully completing the module you will be able to...

• 1. Apply knowledge from various scientific disciplines to the identification of potential targets for novel therapies
• 2. Explain the fundamental pharmacological principles that govern drug bioavailability, specificity/selectivity and potency
• 3. Describe and select appropriate methodology to test the effectiveness of potential new drugs
• 4. Describe, and give examples of, therapeutic agents (drugs, biologics etc) that have been developed or modified using a rational approach

ILO: Discipline-specific skills

On successfully completing the module you will be able to...

• 5. Retrieve and evaluate relevant literature in the area of pharmacological sciences
• 6. Identify opportunities for biomedical research based on current understanding
• 7. Develop a plan of research to test a hypothesis in the area of pharmacological science

ILO: Personal and key skills

On successfully completing the module you will be able to...

• 8. Work effectively as part of a team
• 9. Evaluate information and summarise it accurately
• 10. Communicate ideas clearly and concisely by oral and written means

Syllabus plan

Each week will involve expert-provided seminars explaining the important concepts relating to particular tools available for drug development (from pathophysiology to drug delivery and metabolism), along with examples of where these concepts have been relevant in prior drug design. Supplementary to this teaching, laboratory visits and/or computer-based workshops and/or video recordings will be used where appropriate to demonstrate some of these principles in action. Group tutorial sessions will also be held to explore how the information delivered in the lecture can be transferred and applied to an existing clinical science problem through generation of a hypothesis-driven research plan.

Learning activities and teaching methods (given in hours of study time)

Details of learning activities and teaching methods

Formative assessment

Summative assessment (% of credit)

Details of summative assessment

Details of re-assessment (where required by referral or deferral)

Indicative learning resources - Basic reading

Hill and Rang. Drug Discovery and Development: Technology in Transition (2 nd Ed.). Elsevier. Will be provided digitally.

Indicative learning resources - Web based and electronic resources

see ELE

Indicative learning resources - Other resources

see ELE

Key words search

Pharmacology, Drug Design