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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 Seminar – Fragment-based drug discovery (case study)
7 Lead optimisation - challenges
8 Lead optimisation - in vitro DMPK
9 Lead optimisation - In vivo DMPK
10 Seminar – Lead optimisation (case study)
11 Lead optimisation synthesis

Isotopes and Imaging in Drug Discovery
Dr MA Carroll

1 Introduction to radioactivity
2 Positron Emission Tomography - PET
3-4 Preparation of 11C labelled compounds
5 Preparation of 18F labelled compounds - electrophillic
6 Preparation of 18F labelled compounds - nucleophilic
7 Radiochemistry automation
8 Clinical production
9 Other PET radioisotopes - e.g. 68Ga, 64Cu, 89Zr
10-11 Key PET imaging agents

Teaching Methods

Module leaders are revising this content in light of the Covid 19 restrictions.
Revised and approved detail information will be available by 17 August.

Assessment Methods

Module leaders are revising this content in light of the Covid 19 restrictions.
Revised and approved detail information will be available by 17 August.

Reading Lists

Timetable