Admission requirements
Master students of Bio-Pharmaceutical Sciences, Farmacie, Biomedical Sciences, Life Science & Technology and Molecular Science & Technology. Interested students from other Master programs should contact the course coordinator to discuss the possibilities.
Description
Traditional molecular pharmacology concepts such as affinity, potency and selectivity have been the principal foundation for pre-clinical drug development to date. Unfortunately, these molecular concepts do not always directly translate to clinical drug efficacy. Therefore, studying novel molecular pharmacological concepts is necessary to improve the clinical success of drug development.
Since 30% of all approved therapeutics target G protein-coupled receptors (GPCRs), we will focus on this important class of drug targets. In this course, three novel concepts will be introduced: i. drug-target binding kinetics; ii. allosteric modulation; iii. biased agonism.
These novel concepts will be examined using case studies in which marketed drugs are (serendipitously) based on these novel concepts. At the end, these findings will be presented in the form of a written report and an oral presentation.
This course aims to:
Explain the needs for novel concepts in early GPCR drug discovery to improve clinical efficacy.
Show the importance of GPCRs in drug discovery.
Give an overview of the novel concepts in molecular pharmacology used in early GPCR drug discovery.
Give insight in the different in vitro assays that can be used to prove the mechanism of action of novel drugs at GPCRs.
Give students the tools to investigate whether specific therapeutics operate through a novel concept.
Teach students how to find and present (written and oral) scientific data substantiating a novel concept.
Note that these are expert lectures series and that hence the content might change every year.
Course objectives
At the end of this course the student is able to:
Identify the novel concepts in GPCR molecular pharmacology.
Interpret the experimental data that substantiate the mechanism of action (“concept”) of a specific drug and describe the findings in a report as well as an oral presentation.
Explain the differences between the ‘golden standard drug’ and a drug working through a novel concept in a report as well as an oral presentation.
Timetable
This course is scheduled for semester 2, period 4. A detailed course schedule will be published on Brightspace.
Mode of instruction
Lectures, tutorials, group assignments and self-tuition.
Assessment method
The course assessment is based on the written report (50%) and the presentation of this report (50%). For each individual component, the grade is by using a decimal integer between 1.0 and 10.0 that should be ≥ 5.5. The final grade is expressed using an integer between 1 and 10 and can be rounded off/up to a half integer, with the exception of the grade 5.5. Final grades between 5.50 and 5.99 will be rounded up to 6.0. The final grade should be 6.0 to complete this course successfully.
Reading list
Will be announced during the course.
Registration
Application via uSis for both the course and exam is mandatory. Registration for the course closes 14 days before the start of the course or earlier when the maximum number of students is reached. Registration for the exam closes 7 days before the exam date or earlier when the maximum number of students is reached.
Contact
Coordinator: Prof. dr. Laura Heitman (e-mail: l.h.heitman@lacdr.leidenuniv.nl).
Remarks
A minimum of 6 participants and a maximum of 15 participants applies to this course. Placement is based on the registration date.
This information is without prejudice. Alterations can be made for next year.