Drug Discovery

Course code: FMIMM1131U (Previously M-8113)

Course objectives

The overall objective of the course is to provide the student with a general comprehension of the elements involved in modern drug discovery. Today, almost all drug discovery programs are directed towards design of either small molecules or biologics acting selectively at specific targets. As an initial step, the target involved in a given disease has to be identified and validated, which will subsequently lead to design of ligands acting selectively in a desired fashion at the target. During this lead optimization process a growing number of considerations, besides the action at the disease target, have to be taken into consideration such as ADME, toxicology and production issues. Finally, the lead candidates have to show efficacy in relevant animal disease models before the final candidate can enter pre-clinical studies.  In the current course we will focus on the target identification and validation as well as the lead optimization processes.

Target group

The course is intended for MIND students and other professionals working in drug discovery and development who would like to increase their knowledge regarding modern techniques used in target identification & validation and lead optimization.

Prerequisites

Applicants must meet the following criteria:

• A relevant bachelor degree or equivalent
• A minimum of 2 years of relevant job experience
• Proficiency in English

A basic knowledge of gene transcription & translation and the drug discovery process is required, which can be obtained by reading chapter 1 from "Analysis of Genes and Genomes" by Richard J. Reece (Wiley, ISBN 0470843802) and chapter 4 from “Drug Discovery and Development" by Humphrey P. Rang (Churchill Livingstone, ISBN 0443064202), respectively. In addition chapter 5 and 6 of the latter book is required reading for the workshop on the first day. Additional chapters of both books cover many of the subjects of the course and are thus recommended reading (a list of recommended reading will be provided before the course).

Expected learning outcomes

Upon completion of the course, participants are expected to be able to:

Knowledge

• Demonstrate comprehension of target identification and validation methods and processes
• Demonstrate insight into lead optimization methods and processes

Skills

• Apply basic computational methods in the area of bioinformatics and structure based drug design
• Orally present a subject in the drug discovery area (however, this is not part of the assessment)

Competencies

• Conduct a valid scientific literature study in the area of drug discovery
• Write a scientifically based report on drug discovery aspects using scientific literature

Contents

The following topics will be covered in lectures during the course:

• Target classes: receptors, channels, transporters and enzymes
• Target identification using bioinformatics, genetics, proteomics and reverse pharmacology
• Target evaluation using bioinformatics
• Target validation using gene knock-down, knock-out and knock-in technologies
• Structure based drug design
• Drug design aspects related to small molecules and biologics
• Pitfalls in drug discovery and translational aspects going from a molecular target to whole animals
• Case stories

Target prioritization, bioinformatics and structure based drug design will be covered in workshops.

Course materials/syllabus

A basic knowledge of gene transcription & translation and the drug discovery process is required, which can be obtained by reading chapter 1 from "Analysis of Genes and Genomes" by Richard J. Reece (Wiley, ISBN 0470843802) and chapter 4 from “Drug Discovery and Development" by Humphrey P. Rang (Churchill Livingstone, ISBN 0443064202), respectively. In addition chapter 5 and 6 of the latter book is required reading for the workshop on the first day. Additional chapters of both books cover many of the subjects of the course and are thus recommended reading (a list of recommended reading will be provided before the course). The examination report will be based on a literature search performed by the participants and there is therefore no common syllabus for the course.

Teaching methods

The course is organized as an intensive 5-day course and will comprise approximately 20 lectures, 4 afternoon workshops and an afternoon with student presentations.

Assessment

Type of examination: A written report to be submitted after the course. Deadline: Monday January 2, 2012 at 4 PM

Examination design: A written report based on a case story. The examination report must be based on original peer-reviewed scientific articles found by literature search performed by the participants and there is therefore no common syllabus for the course. The participants will be introduced to literature searches during the course and the examination report is typically based on 20-40 articles.

Assessment: According to the 7-point grading scale.

Examiner(s): Course director and external examiner.

Grading

Grade 12

The participant:

• writes a report in his/hers own words, which demonstrates an exhaustive literature search and the most important literature relevant for the selected case has been properly referenced.
• demonstrates an ability to analyze, recapitulate and critically evaluate the most important literature for the selected case.
• demonstrates a correct use of the terms used in the field of drug discovery.
• demonstrates that he/she masters the central concepts in the field of drug discovery and has an ability to combine the disciplines with each other in the analysis of the selected case.
• writes a coherent report, which within the size limit provides an excellent balance of the various sub-topics of the selected case. 

Grade 7

The participant:

• writes a report in his/hers own words, which demonstrates a throughout literature search and important literature relevant for the selected case has been properly referenced.
• demonstrates an ability to analyze and recapitulate relevant literature for the selected case.
• demonstrates a fairly correct use of the terms used in the field of drug discovery.
• demonstrates that he/she masters the central concepts in the field of drug discovery and has an understanding of the disciplines relevant for the selected case.
• writes a coherent report, which within the size limit provides a proper balance of the various sub-topics of the selected case.

Grade 02

The participant:

• writes a report in his/hers own words, which demonstrates an satisfactory literature search and some important literature relevant for the selected case has been referenced.
• demonstrates an ability to understand and report relevant literature for the selected case.
• demonstrates knowledge of the terms used in the field of drug discovery.
• demonstrates an understanding of the central concepts and disciplines relevant for the selected case.

Student workload

Preparation: 15 hours
Confrontation: 40 hours
Preparation of student presentations: 7 hours
Writing of assessment report: 20 hours
In total: 82 hours

Course directors

Professor Hans Bräuner-Osborne and associate professor Rasmus P. Clausen, Department of Medicinal Chemistry, The Faculty of Pharmaceutical Sciences.

Lecturers

This list of lecturers may be subject to change.

• Peter Høngaard Andersen, H. Lundbeck
• Hans Bräuner-Osborne, University of Copenhagen
• Harald S. Hansen, University of Copenhagen
• Rasmus P. Clausen, University of Copenhagen
• Lotte Bjerre Knudsen, Novo Nordisk
• Michael Lees, BRIC/University of Copenhagen
• Bo Hansen, Santaris
• Ulrik Svane Sørensen, NeuroSearch
• Cord Brakebusch, BRIC/University of Copenhagen
• Nicole Schmitt, University of Copenhagen
• David Gloriam, University of Copenhagen
• Klaus Bøgesø, H. Lundbeck
• Thomas Balle, University of Copenhagen
• Torben Hansen, University of Copenhagen
• Kristian Strømgaard, University of Copenhagen
• Niels Plath, H. Lundbeck
• Thomas Høeg-Jensen, Novo Nordisk

Practical information

Status: Master's level (second-cycle). Compulsory for MIND students, elective for other part-time master's students at the Faculty of Pharmaceutical Sciences (subject to study board approval) and open for freelance students who meet the admission criteria.

Date: 5-9 December 2011. Deadline for submission of written report: Monday January 2, 2012 at 4 PM

Application deadline: 1 October 2011. Closed for applications.

Course credits: 3 ECTS credits = a student workload of approx. 82 hours

Course fee: Part-time master’s students at Faculty of Pharmaceutical Sciences DKK 8,950, freelance students DKK 10,700, freelance students from non-EU/EEA countries DKK 13,550. An additional fee of DKK 1,000 will be charged for course materials and lunch. Prices may be subject to change. Books must be purchased by the participants.

Course capacity: 25 participants.

Language of instruction: English.

Approved by the MIND/MPRA Study Board 26 August 2010.