Module Details

The information contained in this module specification was correct at the time of publication but may be subject to change, either during the session because of unforeseen circumstances, or following review of the module at the end of the session. Queries about the module should be directed to the member of staff with responsibility for the module.
Title Foundations of Medicinal Chemistry
Code CHEM141
Coordinator Dr JW Gaynor
Chemistry
J.W.Gaynor@liverpool.ac.uk
Year CATS Level Semester CATS Value
Session 2018-19 Level 4 FHEQ First Semester 15

Pre-requisites before taking this module (or general academic requirements):

A level Chemistry or equivalent here 

Aims

The aim of this module is to provide students with and understanding of :
1. The key components of cells that act as the building blocks for the key macromolecular structures that are essential in medicinal chemistry.
2. How macromolecules interact with each other to allow for natural cellular processes (such as gene expression) that can be exploited by medicinal chemists
3. The key drug targets in medicinal chemistry

Learning Outcomes

Upon successful completion of this module, a student will be able to demonstrate an understanding of the chemical components of cells.

Upon successful completion of this module, a student will be able to demonstrate an understanding of the structure, chemical bonding and interactions of a range of cellular macromolecules that allow natural cellular processes to occur

Upon successful completion of this module, a student will be able to demonstrate an understanding of the key drug targets in medicinal chemistry, including enzymes, receptors and nucleic acids


Teaching and Learning Strategies

Lecture - The module consists of 28 lectures (45-50 minutes) which will be used to provide the background material necessary to succeed in this module. The learning approach will employ a mixture of traditional delivery alongside components with prior student engagement consisting of pre-recorded video captures to allow in class discussions of worked examples. The lecture component will be used as the main source of interaction with students.

Tutorial - In addition to the lecture series, there will be a series of tutorials to support the various pieces of coursework which will be evenly split between the cell biology and medicinal chemistry components of the course. Tutorials will give students the opportunity to raise specific or more general issues to cover areas of ambiguity.


Syllabus

The course will have the following syllabus, but there is likely to be overlap in the delivery of the two sections.
 
FOUNDATIONS OF CELL BIOLOGY
Lectures 1-6 (Introduction to cell biology, chemical components of cells and related thermodynamics)
  • Non-covalent interactions, energy and the properties of water.
  • Unity and diversity of cells
  • Model organisms
  • How we look at cells
  • Components of cells: Sugars, fatty acids, amino acids and nucleotides
  • Macromolecules in cells: A focus on non-covalent interactions
Lectures 7-10 (DNA, chromosomes, replication and repair)
  • The structure and function of DNA
  • The structure of eukaryotic chromosomes
  • The regulation of chromosome structure
  • DNA replication
  • DNA repair
  • Intercalators and alkylating reagents
Lectures 11-13 (From DNA to protein: How cells read the genome)
  • Transcription, Translation and Ribozymes
  
WHAT ARE THE PRINCIPLE DRUG TARGETS IN MEDICINAL CHEMISTRY? ENZYMES, RECEPTORS & NUCLEIC ACIDS

Lectures 14-16 (Protein structure and function)
  • The basics of protein structure
  • Functions of proteins
  • The shape and structure of proteins (Interesting examples, protein aggregates and assemblies)
  • How proteins work (Antibodies, Lysozymes, Trypsin, Small molecule cofactors)
  • How proteins are controlled (Allosteric proteins)

Lectures 17-18 (Enzymes; Structure and function)
  • Enzymes as catalysts
  • How do enzymes catalyse reactions
  • The active site of enzymes
  • Substrate binding and binding interactions
  • Acid-base catalysis
  • Basic enzyme kinetics
Lecture 19-21 (Enzymes as Drug Targets)
  • Reversible inhibitors
  • Irreversible inhibitors
  • Allosteric inhibitors
  • Uncompetitive and non-competitive
  • Transition state inhibitors
  • Suicide substrates
  • Medicinal uses of enzyme inhibitors
Lecture 22-24 (Receptors; Structure, function and signal transduction)
  • Role of the receptor
  • Neurotransmitters and hormones
  • Receptor activation
  • Ion channel receptors
  • Ligand gated and voltage gated ion channels
  • Protein coupled recept ors
Lectures 25-26 (Receptors as Drug Targets; Agonists and Antagonists)
  • Design of agonists
  • Binding groups
  • The design of antagonists
  • Examples of agonists and antagonists
Lectures 27-28 (Revision)


Recommended Texts

Reading lists are managed at readinglists.liverpool.ac.uk. Click here to access the reading lists for this module.
Explanation of Reading List:

- Alberts'' Essential Cell Biology contains all the relevant cell biology material needed for the first half of the course and has an extensive online resource centre.

- Patrick''s Medicinal Chemistry is the core medicinal chemistry textbook that students will use in future medicinal chemistry programmes (CHEM248/CHEM335, for example). There are also extensive online resources for instructors and students, including online MCQ tests that will be used as formative assessment.


Teaching Schedule

  Lectures Seminars Tutorials Lab Practicals Fieldwork Placement Other TOTAL
Study Hours 28
The module consists of 28 lectures (45-50 minutes) which will be used to provide the background material necessary to succeed in this module. The learning approach will employ a mixture of traditional delivery alongside components with prior student engagement consisting of pre-recorded video captures to allow in class discussions of worked examples. The lecture component will be used as the main source of interaction with students.
  6
In addition to the lecture series, there will be a series of tutorials to support the various pieces of coursework which will be evenly split between the cell biology and medicinal chemistry components of the course. Tutorials will give students the opportunity to raise specific or more general issues to cover areas of ambiguity.
      34
Timetable (if known)              
Private Study 116
TOTAL HOURS 150

Assessment

EXAM Duration Timing
(Semester)
% of
final
mark
Resit/resubmission
opportunity
Penalty for late
submission
Notes
Unseen Written Exam  120  Semester 1 examination period  80  Yes  Standard UoL penalty applies  The final exam 
CONTINUOUS Duration Timing
(Semester)
% of
final
mark
Resit/resubmission
opportunity
Penalty for late
submission
Notes
Coursework  6 hours of in class   Semester 1  20  No reassessment opportunity  Standard UoL penalty applies  Tutorial submissions There is no reassessment opportunity, Work completed in tutorials is primarily formative in nature and hence learning outcomes are covered by the formal resit examination which would contribute 100% of the resit marks if a students failed this component. Notes (applying to all assessments) Each piece of tutorial work / coursework will be spread across the semester to allow for effective timing and will be completed by a variety of either electronic or paper submission. The material in the coursework component will be tailored to align with the the types of problems encountered in the final exam. The coursework will be assessed via a mixture of face-to-face and in class discussion, allowing for direct and immediate feedback, tutorial work submission with written feedback for later reflection and the use of online tests with immediate feedback. For these reasons, the tutorial work cannot be marked anonymously.