Drug discovery part I

PHAR72002 Drug discovery part I 15 Semester 2 Postgraduate Taught Level 7 Division of Pharmacy and Optometry 1 FHEQ level (Framework for Higher Education Qualifications) ' Masters/Integrated Masters P4 ' European Credit Transfer & Accumulation System Rating : 7.5 Students will be introduced to the drug discovery process. You will learn and put into practice concepts relating to target identification, lead identification and optimisation, pre-clinical and clinical studies – considering both the models used in the development of new drugs and how by understanding the relationship between molecular structure and biological properties can be applied to design new drugs. You will learn how genomic approaches as well as bioinformatics resources and tools are used in the process of anticancer drug development.  Students will be introduced to the drug discovery process. You will learn and put into practice concepts relating to target identification, lead identification and optimisation, pre-clinical and clinical studies – considering both the models used in the development of new drugs and how by understanding the relationship between molecular structure and biological properties can be applied to design new drugs. You will learn how genomic approaches as well as bioinformatics resources and tools are used in the process of anticancer drug development.  The unit aims to enable students to:Understand the drug discovery process for small molecule therapeutics and how molecules interact with key biological systems involved in drug efficacy and safety.  Understand some of the key experimental techniques applied to lead discovery and optimisation.  Apply this understanding to look at key approaches to optimising binding, pharmacokinetics and toxicology of compounds.  Compare several current and historical approaches to hit finding.  Provide an understanding of the processes of developing cell‐active drug leads and early validation of new targets in the rational design of novel chemotherapeutic drugs based on their mechanism of action.  Describe, with examples, the drug discovery process for small molecule anticancer therapeutics.Describe the key chemical processes determining physical properties and protein-ligand interaction and apply these to explain the biological activity, pharmacokinetics and toxicology of drug molecules.Compare and contrast the application of techniques such as analogue synthesis, structure-inspired design, SAR transfer, property-based design and other lead optimisation techniques.Describe the advantages and disadvantages of experimental hit finding techniques such as phenotypic screening, fragment-based screening, high throughput screening, DNA-encoded libraries, rational design, fast-follower and other lead discovery techniques.Critique and conduct drug discovery projects through; a) understanding critical attributes of a successful small molecule drug discovery program as it advances through the drug discovery and development process; b) applying this understanding to rationalise the discovery of a number of approved anti-cancer medicines through taught case studies and workshops; and c) understanding the increasingly complex chemical approaches employed in emerging modalities including ADCs, Protacs and RNAi therapies.  Apply fundamental principles (relating to compound properties) to understand complex problems (for example biological activity)Interpret, critique and synthesise existing information to create a reportStructure ideas in a clear and coherent mannerDemonstrate critical thinking and reflection  Develop skills in pharmacophore recognition, SAR analysis and compound design/optimisation.  Gather and retrieve information relating to approved drugsUndertake independent study and manage time appropriatelyEngage in academic discussions and communicate complex ideas and argumentsShow initiative and self-direction in academic and professional development  This module will be delivered in a face-to-face format over 3 weeks (block 3). Teaching material, including lectures that will be available online either prior to face-to-face (F2F) teaching sessions/tutorials or after live/F2F delivery. The face-to-face time will consist of a series of lectures and workshops in which core concepts (introduced through pre-reading) will be re-capped and any further development discussed.  When possible, lectures will be recorded and distributed online.  Alongside this, online discussions and (online and F2F) surgeries will be made available and timetabled for students with academic staff. Associated with each key concept will be a practical exercise to assess the understanding of the students. A mock exam will be provided, and examiners will explain what they look for in the assessments.  1 Written exam 50% 2 Written assignment (inc essay) 50% Individual feedback via Canvas.  N Lectures 12 Practical classes & workshops 56 82