MPS5103 · Drug design and optimisation

Overview

This unit introduces you to pharmaceutical discovery and development, and the strategies used to optimise bioactive molecules into clinically useful drugs. The unit will discuss the sources of bioactive molecules and the approaches used to identify small molecules that interact with a given target (hits); strategies used to optimise properties of hits to give molecules worthy of further development (leads); biological drugs; and the processes by which candidate drugs are evaluated. The unit will provide an introduction to computational modelling and discuss how computer-aided molecular modelling can be used in ligand-based and receptor-based approaches to aid drug development. Throughout the unit, you will be guided through a series of written research exercises, culminating in a comprehensive report on the design and optimisation of a contemporary drug. Upon completing this unit, you will have a knowledge base from which you can critically evaluate the suitability of drug discovery and design approaches appropriate for different situations.

Offerings

Assessment

The Handbook does not list a final examination among the assessment items. That is not a guarantee there is none.

Assessment details may change. Please refer to the assessment information in Moodle closer to the start of the teaching period.

Requisites

The Handbook lists no prerequisite, corequisite or prohibition for this unit.

Learning outcomes

1. Describe the key components and strategies of drug discovery and optimisation
2. Utilise different computational techniques to aid the design of small molecules with good affinity for biomolecular targets
3. Propose modifications to hit molecules necessary to map their structure-activity relationship (SAR), and guide hit-to-lead and lead-to-drug optimisation strategies
4. Critically evaluate different drug discovery and optimisation approaches and identify the most suitable approach for a particular situation
5. Use effective written communication skills to present informed outcomes of enquiry-based research into examples of drug design and optimisation.

Workload

• 36 hours of online modules • Twelve 2-hour workshops • Twelve 1-hour applied sessions • 72 hours of independent study

Student experience, not official rules. Nothing here changes what the Handbook says.