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Module

CHY8421 : Advanced Methods in Drug Discovery

  • Offered for Year: 2020/21
  • Module Leader(s): Dr Ian Hardcastle
  • Other Staff: Dr James Knight
  • Owning School: Natural and Environmental Sciences
  • Teaching Location: Newcastle City Campus
Semesters
Semester 1 Credit Value: 10
ECTS Credits: 5.0

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

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

1 Introduction to radioactivity       , modes of Decay (α, β, γ), 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

Please note that module leaders are reviewing the module teaching and assessment methods for Semester 2 modules, in light of the Covid-19 restrictions. There may also be a few further changes to Semester 1 modules. Final information will be available by the end of August 2020 in for Semester 1 modules and the end of October 2020 for Semester 2 modules.

Teaching Activities
Category Activity Number Length Student Hours Comment
Guided Independent StudyAssessment preparation and completion144:3044:30Independent study and background reading of topics
Guided Independent StudyAssessment preparation and completion25:0010:00Online - feedback on formative coursework, case studies (co-taught with CHY8821)
Structured Guided LearningLecture materials201:0020:00A combination of short recordings of lecture material and text published on VLE each week
Structured Guided LearningLecture materials20:301:00Module introduction and recap. Familiarise yourself with the topics, and recommended reading lists
Scheduled Learning And Teaching ActivitiesWorkshops41:004:00Online - feedback on formative coursework, case studies (co-taught with CHY8821)
Guided Independent StudyIndependent study210:0020:00Online coursework (2 x 50%)
Scheduled Learning And Teaching ActivitiesModule talk10:300:30Online - a short online session given by a lecturer introducing topics
Total100:00
Jointly Taught With
Code Title
CHY8821Modern Methods in Drug Discovery
Teaching Rationale And Relationship

Key concepts and supporting examples are delivered by online lecture materials.

Assessment Methods

Please note that module leaders are reviewing the module teaching and assessment methods for Semester 2 modules, in light of the Covid-19 restrictions. There may also be a few further changes to Semester 1 modules. Final information will be available by the end of August 2020 in for Semester 1 modules and the end of October 2020 for Semester 2 modules.

The format of resits will be determined by the Board of Examiners

Other Assessment
Description Semester When Set Percentage Comment
Written exercise1M50Summative assessment of lecture materials
Written exercise1M50Summative assessment of lecture materials
Formative Assessments
Description Semester When Set Comment
Written exercise1MCoursework exercises
Assessment Rationale And Relationship

The coursework will assess the students’ ability to understand and apply their learning to relevant case studies in drug discovery and imaging.

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.

Reading Lists

Timetable