Admission requirements
Master students of Bio-Pharmaceutical Sciences, Pharmacy, 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 thus 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, and why they are beneficial to drug discovery.
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 1, period 1.
You will find the timetables for all courses and degree programmes of Leiden University in the tool MyTimetable (login). Any teaching activities that you have sucessfully registered for in MyStudymap will automatically be displayed in MyTimetable. Any timetables that you add manually, will be saved and automatically displayed the next time you sign in.
MyTimetable allows you to integrate your timetable with your calendar apps such as Outlook, Google Calendar, Apple Calendar and other calendar apps on your smartphone. Any timetable changes will be automatically synced with your calendar. If you wish, you can also receive an email notification of the change. You can turn notifications on in ‘Settings’ (after login).
For more information, watch the video or go to the 'help-page' in MyTimetable. Please note: Joint Degree students Leiden/Delft have to merge their two different timetables into one. This video explains how to do this.
A detailed schedule of the course will be published on the Brightspace course module.
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%), both which contain an individual aspect.
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.
The time and manner of the inspection and of the feedback session on the examination are specified in the Brightspace module of the course.
Reading list
Will be announced during the course.
Registration
Every student has to register for courses with the enrolment tool MyStudymap. There are two registration periods per year: registration for the fall semester opens in July and registration for the spring semester opens in December. Please see this page for more information.
Please note that it is compulsory to register for every exam and retake. Not being registered for a course means that you are not allowed to participate in the final exam of the course. If you want to retake the exam of the course without following the lectures, you have to contact the coordinator of the course to see if this is possible (you would have passed the other assignments of the course in the earlier year).
Registration for your (resit) exam participation is possible until ten days before the exam.
Extensive FAQ's on MyStudymap can be found here.
Contact
Coordinator: Prof. dr. Laura Heitman (e-mail: l.h.heitman@lacdr.leidenuniv.nl)
Remarks
A minimum of 8 participants and a maximum of 40 participants applies to this course. Placement is based on the registration date in MyStudymap.
This information is without prejudice. Alterations can be made for next year.
Software
Starting from the 2024/2025 academic year, the Faculty of Science will use the software distribution platform Academic Software. Through this platform, you can access the software needed for specific courses in your studies. For some software, your laptop must meet certain system requirements, which will be specified with the software. It is important to install the software before the start of the course. More information about the laptop requirements can be found on the student website.