High-Throughput Screening

Course manual 2024/2025

Course content

In depth study on the bioanalytical, biochemical, pharmacological, and biological screening aspects in pharmaceutical high throughput screening settings related to screening large compound libraries, bioactive extracts, and other bioactive mixture samples in hit-to-lead discovery pipelines in the drug discovery process.

During this course, the potential of modern analytical and biological screening techniques used in target, hit and lead discovery will be discussed. The emphasis will be on the treatment of advanced sample preparation techniques (i.e. automation, high-throughput / combinatorial chemistry, miniaturization), biological and biochemical high throughput screening assays, and advanced analytical bioaffinity profiling methods. Also, the so called “Omics” will be discussed (e.g. proteomics and metabolomics). Bioactivity profiling techniques for screening bioactive mixtures will be discussed and in this regard the integration of analytical separation methods, bioassays, and mass spectrometry into single high throughput profiling platforms will get ample attention.  These techniques will be discussed in relation to pharmacokinetic studies and the applicability of the various techniques within the various stages of target discovery, hit screening, ADME(tox), and early lead discovery. Also, miniaturization and automation approaches in HTS settings will be dealt with.

Study materials

Other

• PDFs and PowerPoint presentations provided via Canvas and/or accessible via the internet (links will be given).

   

  Lectures and tutorials:

   

  Please see the documents in Canvas. The PowerPoint presentation named "HTS Course Overview" gives a detailed explanation/overview of the lectures, tutorials and course structure.

   

  Course reading:

   

  All PowerPoint lectures will be placed in Canvas at least one day before each lecture. All other PDF literature (e.g. academic research papers and reviews) can already be found in Canvas and/or links are given to access the literature. 

Objectives

• Can explain in detail the potential of modern analytical and biological screening techniques used in target, hit and lead discovery.
• Can explain in detail and be able to apply advanced sample preparation techniques in automation and high throughput screening techniques and assay principles in biological and immunological assays.
• Can explain the basics of metabolomics and proteomics approaches in relation to high throughput screening and pharmacokinetic studies.
• Have a basic understanding in miniaturization approaches related to HTS and screening in general.
• Understands and can explain the principles and workflows of the main methods for profiling bioactive mixtures to identify bioactive compounds.
• Design (balance and discriminate between methods) a hypothetical screening campaign plan with background rational and plan of operation.
• Write a report on a hypothetical screening campaign plan with background rational and plan of operation.
• Orally present a hypothetical screening campaign plan with background rational and plan of operation.
• The student will be able to list, describe, compare and understand the topics mentioned in the course content.

Teaching methods

• Lecture
• Presentation/symposium
• Self-study
• Working independently on e.g. a project or thesis

The course starts with a thorough explanation of all subjects that will be discussed, and during which lecture. All students will also work in small groups on an assignment related to a topic in high throughput screening. This assignment results in a group report document and a PowerPoint group presentation. For the group presentation and the preparation of the group report document, students will work in small groups.

Learning activities

Attendance

This programme does not have requirements concerning attendance (TER part B).

Additional requirements for this course:

Absence needs to be communicated to the course coordinator.

Assessment

Examination is in the form of a written examination accounting for 50% of the final mark. All lectures and all literature provided are included in the examination. 

De group presentations on a HTS topic followed by questions and replies to these questions constitutes 25% of the final mark. The group report and the presentation’s topic are dealing with the same topic. The group report document constitutes the other 25% of the final mark. The partial marks for the examination, the presentation and discussion afterwards, and the assignment document all have to be sufficient (>5.5).

Assignments

De group presentations on a HTS topic followed by questions and replies to these questions constitutes 25% of the final mark. The group report and the presentation’s topic are dealing with the same topic. The group report document constitutes the other 25% of the final mark. The partial marks for the presentation and discussion afterwards, and the assignment document all have to be sufficient (>5.5).

Fraud and plagiarism

The 'Regulations governing fraud and plagiarism for UvA students' applies to this course. This will be monitored carefully. Upon suspicion of fraud or plagiarism the Examinations Board of the programme will be informed. For the 'Regulations governing fraud and plagiarism for UvA students' see: www.student.uva.nl

Course structure

Additional information

Recommended prior knowledge: Basic knowledge of biochemistry, separation sciences, spectroscopy and
mass spectrometry.

Contact information

Coordinator

• Jeroen Kool