Chemistry & Disease II - Advanced Medicinal Chemistry - CHE00014H

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  • Department: Chemistry
  • Module co-ordinator: Prof. Marek Brzozowski
  • Credit value: 10 credits
  • Credit level: H
  • Academic year of delivery: 2018-19

Module summary

This module builds on the material introduced in CD1 to consider more advanced aspects of human health and disease. Some aspects - but covered in depth - of complex diseases, role of metals in disease, and modern approaches to drug design will be discussed.

Module will run

Occurrence Teaching cycle
A Autumn Term 2018-19

Module aims

This module builds on the material introduced in CD1 to consider more advanced aspects of human health and disease. The first part will cover several novel elements of Medicinal Inorganic Chemistry with its application in formulation of new metallo-drugs and isotope-containing chemical tools. The second part will be in-depth presentation of modern methods in drug discovery and their application in development of new therapeutic molecules. The module will end with survey of the complexity, and intertwined nature of some common diseases like diabetes, cancer, obesity and aging. It will be illustrated how modern protein chemistry and chemical biology methods provide insight into the role of hormonal control in health and disease, and how complex disease require multi directional therapeutic attacks, and holistic view of human physiology.

Module learning outcomes

  • to understand the importance of inorganic chemistry in biomedical applications
  • to understand the chemical and macromolecular complexity of common diseases such diabetes, cancer and neurodegeneration
  • to understand the methods and application of modern drug discovery processes

Module content

Topics:

Metals in Medicine:

This module will consist of three parts:

(i) The essentiality of elements and the principle of Paracelsus: from metal deficiency and disease to toxic effect of metals. Many 'inorganic' elements are essential for life but may be poisonous. Hence principles for the design of specific metal chelators for the treatment of metal overload will be discussed. (ii) Metals as therapeutic agents: chemotherapy with essential and nonessential elements. This part will focus on recent developments relating to platinum anticancer and gold antiarthritic drugs. (iii) Radiopharmaceuticals and MRI (magnetic resonance imaging) agents as diagnostic tools. By using the right ligands, the toxicity of some metal complexes can be controlled ensuring their gram quantities-applications as MRI contrast agents. Specific ligands allow the tissue/organ targeting of such paramagnetic ions and their radiodiagnostic or radiotherapeutic isotopes.

AKDK

6 lectures

+ 1x2 h

workshop

Molecular Aspects of Complex Diseases:

The main themes of the module are complex diseases that result form the disruption of the inter-cell flow of information. The regulation of cell-cell communication by hormone activated transcription factors, and its clinical modifications will be discussed on examples of nuclear receptors (NRs). Next, the malfunction of classical hormone:membrane receptor signalling will discussed for insulin case (Type 1 and 2 Diabetes). The strategies for insulin replacement and combat of Type 2 Diabetes will be covered.

The impact of protein aggregation on human health (e.g. Alzheimer, Huntington's) will be outlined. The module ends with a survey of up-to-date key molecular issues related to one of the most complex diseases: cancer.

AMB

6 lectures

+ 1x2 h

workshop

Modern Approaches to Drug Discovery:

This module will provide an understanding of the contribution chemical methods and thinking make to the drug discovery process, including target identification, hit identification and lead optimisation. The target-oriented approach to therapeutic intervention will be illustrated with examples from the molecular and cell biology (influenza, HIV, diabetes, obesity, Alzheimer’s and cancer). The examples will also show how a broad range of chemical, biological, structural and computational techniques are being applied in drug discovery. A recurring theme is the need for an understanding of the required properties for a drug molecule. This includes an appreciation of the biological processes that determine ADME and toxicity properties and the types of assays that are used to monitor these.

REH

6 lectures

+1 x 3 h

workshop

Prerequisites

Chemistry Core Modules 1-4, option module CD1 is strongly recommended

Assessment

1.5 h written paper (70%) plus one continuous assessment (30%) based on REH 3 hr workshop.

The continuous assessment is work based on REH workshop. It will probe the understanding of basics of drug design, and will require to use molecular graphics introduced during the workshop.

Assessment

Task Length % of module mark
Essay/coursework
Continuous Assessment
N/A 30
University - closed examination
Chemistry & Disease II: Advanced Medicinal Chemistry
1.5 hours 70

Special assessment rules

None

Additional assessment information

Reading List will be provided by the module tutor

Reassessment

Task Length % of module mark
University - closed examination
Chemistry & Disease II: Advanced Medicinal Chemistry
1.5 hours 70

Module feedback

The closed examinations are marked typically within 10 days with mark slips (with per-question break-down) being returned to students via supervisors. Outline answers are made available via the Chemistry web pages when the students receive their marks, so that they can assess their own detailed progress/achievement. The examiners reports for each question are made available to the students via the Chemistry web pages.

Feedback for the coursework will be delivered in the same time as the examiners reports.

Indicative reading

The key texts will be provided during the courses by the lecturers.



The information on this page is indicative of the module that is currently on offer. The University is constantly exploring ways to enhance and improve its degree programmes and therefore reserves the right to make variations to the content and method of delivery of modules, and to discontinue modules, if such action is reasonably considered to be necessary by the University. Where appropriate, the University will notify and consult with affected students in advance about any changes that are required in line with the University's policy on the Approval of Modifications to Existing Taught Programmes of Study.