High-Throughput Screening

Course manual 2018/2019

Course content

In depth study on the bio-analytical and the biological screening aspects related to target discovery and hit and lead discovery of drugs.

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 immunological high throughput screening assays and advanced separation methods. Also, the so called “Omics” will be discussed (e.g. proteomics and metabolomics). These techniques will be discussed in relation with pharmacokinetic studies and the applicability of the various techniques within the various stages of target discovery, hit screening, ADME(tox), and early lead discovery. Finally, miniaturization approaches 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 PDF e-book chapters and other literature (e.g. academic research papers and reviews) can already be found in Canvas and/or links are given to access the literature. It will be announced when each PDF literature is/are to be read in order to prepare for a respective lecture.

Objectives

The student:

• 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 troughput 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
• Has 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
• Can design (balance and discriminate between methods) a hypothetical screening campaign plan with background rational and plan of operation
• Can write a report on a hypothetical screening campaign plan with background rational and plan of operation
• Can orally present a hypothetical screening campaign plan with background rational and plan of operation

Teaching methods

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

The course starts with a thorough explanation on all subjects that will be discussed, and during which lecture. During the lectures, relevant literature per lecture will be mentioned. This literature is mainly from e-books (chapters) and from academic papers/reviews. All literature that will be mentioned can be found in Canvas. All this literature has to be studied for the examination. All students will work on an assignment related to a topic in high throughput screening. This assignment results in a document and a PowerPoint presentation for which students will work in a small group.

Learning activities

Attendance

The programme does not have requirements concerning attendance (OER-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. All material to be studied and learned for the examination can be accessed during the examination, except the PDFs of all lectures. Students can take all printed material and/or a computer with them during the examination. The use of internet during the examination is not allowed.

(Depending on the number of students entering the re-take examination, optionally oral re-take examinations can be given)

De presentation of 4 minutes per student followed by questions and replies to these questions constitutes 25% of the final mark. The Document’s topic and the presentation’s topic are related to each other. The document is between 5 and 7 pages (Times New Roman type 12; line spacing 1) per student excluding title page, index and references, and with a maximum of 3 Figures/Tables per student. The assignment document constitutes the other 25% of the final mark. The marks for the examination, the presentation and discussion afterwards, and the assignment document all have to be sufficient (6.0).

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