FaF:CORE048 Drug Design - Course Information

CORE048 Drug Design is not about a Fashionable Drug Box

Extent and Intensity

2/0/0. 3 credit(s). Type of Completion: k (colloquium).

Teacher(s)

doc. PharmDr. Oldřich Farsa, Ph.D. (lecturer)
RNDr. Eva Havránková, Ph.D. (lecturer)
Mgr. Veronika Murgašová (lecturer)
PharmDr. Magdaléna Onuščáková (lecturer)
Mgr. Anna Ruprechtová (lecturer)

Guaranteed by

doc. PharmDr. Oldřich Farsa, Ph.D.
Department of Chemical Drugs – Departments – Faculty of Pharmacy
Supplier department: Department of Chemical Drugs – Departments – Faculty of Pharmacy

Timetable

Mon 8:00–9:40 44-037

Prerequisites

FAKULTA(LF) || FAKULTA(FF) || FAKULTA(PrF) || FAKULTA(FSS) || FAKULTA(PřF) || FAKULTA(FI) || FAKULTA(PdF) || FAKULTA(FSpS) || FAKULTA(ESF)
Fundamentals of chemistry, biology, and physics on the secondary school level; fundamentals of European and world history

Course Enrolment Limitations

The course is offered to students of any study field.
The capacity limit for the course is 100 student(s).
Current registration and enrolment status: enrolled: 13/100, only registered: 0/100, only registered with preference (fields directly associated with the programme): 0/100

Course objectives

The aim of the course is to introduce the general university public to the view of the drug as its own effective molecule and to acquaint students with the path that leads to the discovery of the drug and its introduction into medical practice. From the perspective of historical development, current state and future perspectives, the course describes the sources of biologically active molecules and how these original "lead compounds" can be improved and optimized so that they can serve as effective and safe drugs for the present and future. It also focuses on the difference between "small molecules", ie classic "chemical" drugs, and "large" molecules, so-called bio-drugs, whose importance in the treatment of serious diseases has increased significantly in recent decades. The course also describes the role of chemical, biological, mathematical, physical, computer, and other disciplines in drug development, and mentions, among other things, the use of computer modeling of potentially effective molecules and their interactions with the target structure, such as receptor or enzyme active site in virtual space. The intended "side effect" of the course is also to increase the visibility of the Faculty of Pharmacy among Faculties of MU, and also the reputation of pharmacy as a profession in society.

Learning outcomes

After passing this course, the student will be expected to know among others:
-main moments and persons of history drug research and development in Czech, European and world context
-differences between classical "small molecule" drugs and "biologics"
-differences between original drug products and generics, and between originator products and biosimilars -meaning of the concept of the "lead compound", possible resources of them, and possible ways how to optimize them
-biomolecules that are used as drug targets (enzymes, receptors, nucleic acids...)
-basic fundamentals of mathematical, statistical, computer-aided and other rational theoretical methods used in drug design
-a basic overview of synthetic and other methods how used and experimental drugs are prepared
-and many others

Syllabus

• The name of every topic is followed by the initials of the lecturer: VB = Veronika Ballayová; EH = Eva Havránková; OF = Oldřich Farsa; MO = Magdalena Onuščáková; AR = Anna Ruprechtová
• Topics are preliminary; they can be modified
• 1. The fate of the drug in the body – why it is important? (ADME) EH
• 2. The fate of the drug in the body. Is the design of the box of medicines important? EH
• 3. The path of the drug over time – from idea to the patient VB
• 4. Drug patents and copying: generics versus biosimilars. (When two do the same, it needs not to be the same.) OF
• 5. World famous scientists and their breakthrough discoveries MO 6. How much did Alexander Fleming discover penicillin? "World" and "our Czech" penicillin. (Penicillin – facts and falsehoods) OF
• 7. Treatment procedures in history - did it really work? VB
• 8. Famous pharmaceuticals – Curious stories of their origin MO
• 9. Czech scientists and their world-class discoveries EH (could be putted together with No.5 - World famous scientists)
• 10. Statistics in drug research: fundamentals of classical quantitative structure-activity relationships (QSAR) methods. (QSAR, statistics, and their role in the design of drugs) OF
• 11. Large molecules as drugs: artificial antibodies, modified receptors, and pieces of altered nucleic acid as drugs. OF
• 12. In silico and modeling experiments in the design of new drugs. What are privileged structures? MO
• 13. Neural networks in science and the latest trends in the Medicinal Chemistry and Drug Design EH
• 14. You ask, we answer. Free discussion about Drug Design and Medicinal Chemistry

Literature

• Mykoin ph510. A played film - "docudrama" devoted to the development of the original Czech penicillin under conditions of German occupation. Czechoslovakia, 1963, available at YouTube at https://youtu.be/qSrQXdXDExw
• Bickel, Lennard. Florey: The man who made penicillin. Bloomsbury Publishing, 2015
• BLASS, Benjamin E. Basic principles of drug discovery and development. Second edition. London: Academic Press, 2021, xvii, 718. ISBN 9780128172148. info
• KANG, Lydia and Nate PEDERSEN. Quackery: a brief history of the worst ways to cure everything. New York: Workman Publishing, [2017]. ISBN 978-0761189817.
• ROCHE, Victoria F., S. William ZITO, Thomas L. LEMKE and David A. WILLIAMS. Foye's principles of medicinal chemistry. 8th edition. Philadelphia: Wolters Kluwer, 2020, xix, 1626. ISBN 9781496385024. info
• CIKRT, Tomáš. Příběhy léků: příručka pro zvídavé čtenáře o vzniku, vlastnostech a používání léků. Praha: Státní ústav pro kontrolu léčiv, 2012. ISBN 978-80-260-1403-4
• KAJAN, Marek. Očami farmácie: 50 otázok, na ktoré určite chcete poznať odpoveď. Bratislava: Petit Press, 2022. ISBN 978-80-559-0770-3.
• Kuchař M., Rejholec V. Využití kvantitativních vztahů mezi strukturou a biologickou aktivitou. Academia,. Praha, 1987. info

Teaching methods

Oral lectures on-line through MS-Tems.

Assessment methods

2 - 3 quizzes randomly during lectures, final exam in the form of a colloquium

Language of instruction

English

Further Comments

Study Materials
The course is taught annually.

• Enrolment Statistics (recent)
  
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