Molecular and Cellular Pharmacology
Module code: BS3054
Module co-ordinator: Professor John Challiss
In this module you will study molecular pharmacology and signal transduction pathways (especially those regulated by GPCRs), including their structure and function in different cells and tissues. Within this framework we will consider the various approaches that have been successfully employed pharmacologically to manipulate different aspects of these pathways and explore future strategies to the treatment of different diseases. In addition to considering classical pathways downstream of GPCRs (e.g. cyclic AMP/cyclic AMP-dependent protein kinase, IP3/Ca2+, DAG/protein kinase C, etc.), we will examine how different receptor superfamilies regulate enzymes/pathways, such as phosphoinositide 3-kinase, mitogen-activated protein kinases and transcription factors. We will also consider various aspects of receptor regulation (e.g. receptor desensitization and internalization). Throughout the module we will discuss the latest research in molecular and cellular pharmacology/cell signalling, looking in particular at new pharmacological approaches to treating disease.
Topics covered
- Basic structures and functions of receptors and key components of signal transduction cascades
- Regulation of receptors by agonists, antagonists, and inverse agonists; how receptor activity can be altered by ligands binding at allosteric as well as orthosteric sites; mechanisms of GPCR desensitisation and its physiological and pharmacological significance
- Signalling pathways: their structure (sub-cellular compartmentation, signalling scaffolds etc.) and physiological function(s); how molecular therapeutic targets can be selected and pharmacologically manipulated
- Pharmacological manipulation of GPCRs, receptor tyrosine kinases, nuclear receptors, ion channels and intracellular enzyme activities
- Acute cell signalling events and their relation to longer-term changes in cell phenotype and fate; cell surface to nuclear signalling and how changes in stimulation patterns or components of signalling pathways may regulate longer term physiological or pathophysiological adaptations as might be observed in certain disease conditions
Learning
- 30 one-hour lectures
- 8 hours of practicals
- 2 one-hour tutorials
Assessment
- Exam, 3 hours (70%)
- Essay, 2,000 words (15%)
- Lab report/data handling exercise (15%)