NES8801 : Modern Methods in Drug Discovery
- Offered for Year: 2023/24
- Module Leader(s): Dr Ian Hardcastle
- Lecturer: Dr Matt Hopkinson, Dr James Knight
- Owning School: Natural and Environmental Sciences
- Teaching Location: Newcastle City Campus
Semesters
Your programme is made up of credits, the total differs on programme to programme.
| Semester 1 Credit Value: | 20 |
| ECTS Credits: | 10.0 |
| European Credit Transfer System | |
Aims
To provide an overview of the methods and approaches used in modern drug discovery. To introduce the key stages of a project i.e. target identification and validation, hit discovery, hit validation, hit-to-lead optimisation and lead optimisation. To familiarise students with the most commonly used synthetic methods in medicinal chemistry. To provide students with an understanding of the role of medical imaging in drug discovery, synthetic methods for the incorporation of radioisotopes into biologically active molecules and the quality control requirements for clinical production.
Outline Of Syllabus
The discovery of new drugs to treat unmet needs of patients is a global undertaking. This module covers modern topics in drug discovery, e.g. target validation, hit identification and the pre-clinical optimisation of drugs, along with the preparation and application of radiopharmaceuticals for imaging and therapy. It is illustrated with case studies from recent discovery projects.
Methods in Drug Discovery
Dr IR Hardcastle
List of topics covered:
1 Overview of drug discovery and drug targets
2 Peptide synthesis and peptide libraries
3 Hit identification technologies
4 Small-molecule library synthesis
5 Hit-to-lead strategies and methods
6 Fragment-based drug discovery
7 Lead optimisation - challenges
8 Lead optimisation - in vitro and in vivo DMPK
10 Lead optimisation – synthesis
11 Case studies
Isotopes and Imaging in Drug Discovery
Dr J Knight
List of topics covered:
1 Introduction to radioactivity , modes of Decay (?, ?, ?), radioactive decay calculations
2 Overview of PET Imaging, dosimetry, common PET radioisotopes
3 Calculating radiochemical yield and molar (radio)activity
4 Radiolabelling with carbon-11
5 Radiolabelling with fluorine-18: electrophilic approach, nucleophilic approach, example
radiotracers
6 Radiolabelling with iodine-124
7 Influence of radiotracer design upon biodistribution and pharmacokinetics
8 PET radiometals: chelation requirements, examples of radiometal-based PET radiotracers
9 PET imaging of hypoxia
10 PET radiotracers as companion diagnostics
11 Radiopharmaceutical Production
Teaching Methods
Teaching Activities
| Category | Activity | Number | Length | Student Hours | Comment |
|---|---|---|---|---|---|
| Guided Independent Study | Assessment preparation and completion | 6 | 5:00 | 30:00 | Preparation for coursework tasks |
| Guided Independent Study | Assessment preparation and completion | 4 | 1:00 | 4:00 | Summative coursework exercises |
| Guided Independent Study | Assessment preparation and completion | 2 | 1:00 | 2:00 | Formative coursework exercises |
| Guided Independent Study | Directed research and reading | 50 | 0:30 | 25:00 | Accessing prerecorded lecture material and background reading |
| Scheduled Learning And Teaching Activities | Small group teaching | 10 | 1:00 | 10:00 | PiP seminars covering course materials |
| Scheduled Learning And Teaching Activities | Drop-in/surgery | 11 | 1:00 | 11:00 | Online drop-in sessions |
| Guided Independent Study | Independent study | 1 | 118:00 | 118:00 | Background reading and practice questions |
| Total | 200:00 |
Teaching Rationale And Relationship
Key concepts and supporting examples are delivered by online teaching materials. Seminars are used to reinforce key concepts, provide additional examples and to provide practice questions. Online quizzes revise and reinforce conceptual understanding.
Written assignments allow students to access and review representative primary literature adding depth to conceptual understanding.
Study Abroad students may request to take their exam before the semester 1 exam period, in which case the format of the paper may differ from that shown in the MOF. Study Abroad students should contact the school to discuss this.
Assessment Methods
The format of resits will be determined by the Board of Examiners
Exams
| Description | Length | Semester | When Set | Percentage | Comment |
|---|---|---|---|---|---|
| Digital Examination | 120 | 1 | A | 50 | MCQ |
Other Assessment
| Description | Semester | When Set | Percentage | Comment |
|---|---|---|---|---|
| Written exercise | 1 | M | 25 | N/A |
| Written exercise | 1 | M | 25 | N/A |
Formative Assessments
Formative Assessment is an assessment which develops your skills in being assessed, allows for you to receive feedback, and prepares you for being assessed. However, it does not count to your final mark.
| Description | Semester | When Set | Comment |
|---|---|---|---|
| Written exercise | 1 | M | 2 x written exercises (1000 words each). Preparation for summative coursework |
Assessment Rationale And Relationship
The online timed 2hr MCQ quiz exam (Inspera) – tests factual knowledge and understanding. Ability to solve calculation based questions. Worth 50%)
2 x written literature based assignments (1000 words). Each is based on literature from the two different subject strands in the module. Each worth 25%
Reading Lists
Timetable
- Timetable Website: www.ncl.ac.uk/timetable/
- NES8801's Timetable